Publications by authors named "Bhupinder Kapoor"

27 Publications

  • Page 1 of 1

Development of mushroom polysaccharide and probiotics based solid self-nanoemulsifying drug delivery system loaded with curcumin and quercetin to improve their dissolution rate and permeability: State of the art.

Int J Biol Macromol 2021 Aug 28;189:744-757. Epub 2021 Aug 28.

Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo, NSW 2007, Australia; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW 2007, Australia.

The role of mushroom polysaccharides and probiotics as pharmaceutical excipients for development of nanocarriers has never been explored. In the present study an attempt has been made to explore Ganoderma lucidum extract powder (GLEP) containing polysaccharides and probiotics to convert liquid self nanoemulsifying drug delivery system (SNEDDS) into solid free flowing powder. Two lipophilic drugs, curcumin and quercetin were used in this study due to their dissolution rate limited oral bioavailability and poor permeability. These were loaded into liquid SNEDDS by dissolving them into isotropic mixture of Labrafill M1944CS, Capmul MCM, Tween-80 and Transcutol P. The liquid SNEDDS were solidified using probiotics and mushroom polysaccharides as carriers and Aerosil-200 as coating agent. The solidification was carried out using spray drying process. The process and formulation variables for spray drying process of liquid SNEDDS were optimized using Box Behnken Design to attain required powder properties. The release of both drugs from the optimized spray dried (SD) formulation was found to be more than 90%, whereas, it was less than 20% for unprocessed drugs. The results of DSC, PXRD and SEM, showed that the developed L-SNEDDS preconcentrate was successfully loaded onto the porous surface of probiotics, mushroom polysaccharides and Aerosil-200.
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http://dx.doi.org/10.1016/j.ijbiomac.2021.08.170DOI Listing
August 2021

Combination therapy of curcumin and fecal microbiota transplant: Potential treatment of polycystic ovarian syndrome.

Med Hypotheses 2021 Sep 15;154:110644. Epub 2021 Jul 15.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, India.

Polycystic ovarian syndrome (PCOS) is a combination of various symptoms like anovulation, hirsutism, chronic amenorrhea, infertility, obesity and polycystic ovaries. It affects over 7 million women worldwide. The current strategy to treat this disorder is based on the use of drugs that provide symptomatic relief. Most of these, however, exhibit numerous side effects and are not able to ameliorate all the signs and symptoms of PCOS. As dysbiosis is considered as one of the prime underlying causes of PCOS, restoration of eubiosis was considered as a plausible way to treat it. Bacteriotherpeutics like probiotics, synbiotics and even fecal microbiota transplant (FMT) have shown considerable effectiveness in PCOS. Of these baceteriotherapeutic options, FMT is considered to be the most holistic as it encompasses the bacteriome, virome, fungome, archaeome and even parasitome while both probiotics as well as synbiotics mainly comprise bacteria. Repeated FMT, however, is not a pragmatic option because of its inconvenience, lack of standardization, involved risk and scepticism amongst patients and physicians. If the eubiosis ushered by FMT is sustained for a long time, the repeated administrations of FMT can be avoided and maintenance therapy with any agent that can maintain the eubiotic condition can be adopted. Role of curcumin on gut microbiota is widely known. It is largely attributed to the ability of certain microbes to consume polyphenols as substrates and its positive effect on bacterial consumption of nutrients such as sugars. Based on various mechanisms and studies, a new hypothesis is being proposed wherein FMT and curcumin combination is predicted to be an effective and sustained treatment of PCOS with much lower rates of remission.
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http://dx.doi.org/10.1016/j.mehy.2021.110644DOI Listing
September 2021

Recent updates on animal models for understanding the etiopathogenesis of polycystic ovarian syndrome.

Life Sci 2021 Sep 23;280:119753. Epub 2021 Jun 23.

Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Australia.

Polycystic ovarian syndrome (PCOS) is the primary cause of female infertility affecting several women worldwide. Changes in hormonal functions such as hyperandrogenism are considered a significant factor in developing PCOS in women. In addition, many molecular pathways are involved in the pathogenesis of PCOS in women. To have better insights about PCOS, it is data from clinical studies carried on women suffering from PCOS should be collected. However, this approach has several implications, including ethical considerations, cost involved and availability of subject. Moreover, during the early drug development process, it is always advisable to use non-human models mimicking human physiology as they are less expensive, readily available, have a shorter gestation period and less risk involved. Many animal models have been reported that resemble the PCOS pathways in human subjects. However, the models developed on rats and mice are more preferred over other rodent/non-rodent models due to their closer resemblance with human PCOS development mechanism. The most extensively reported PCOS models for rats and mice include those induced by using testosterone, letrozole and estradiol valerate. As the pathophysiology of PCOS is complex, none of the explored models completely surrogates the PCOS related conditions occurring in women. Hence, there is a need to develop an animal model that can resemble the pathophysiology of PCOS in women. The review focuses on various animal models explored to understand the pathophysiology of PCOS. The article also highlights some environmental and food-related models that have been used to induce PCOS.
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http://dx.doi.org/10.1016/j.lfs.2021.119753DOI Listing
September 2021

Exploring role of polysaccharides present in Ganoderma lucidium extract powder and probiotics as solid carriers in development of liquisolid formulation loaded with quercetin: A novel study.

Int J Biol Macromol 2021 Jul 17;183:1630-1639. Epub 2021 May 17.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, India.

Ganoderma lucidium extract powder (GLEP) contains various polysaccharides which are well known for their antioxidant and anti-inflammatory actions. Probiotics (PB) are well-established for providing a plethora of health benefits. Hence, use of mushroom polysaccharides and probiotics as carriers to solidify liquisolid formulation is anticipated to function as functional excipients i.e. as adsorbent that may provide therapeutic benefits. Quercetin (QUR) has been used as model lipophilic drug in this study. QUR loaded liquisolid compacts (LSCs) were formulated using Tween 80 as solvent. These were further solidified using a combination of PB and GLEP as carriers. Aerosil-200 (A-200) was used as coating agent. The formulation exhibited very good flow characteristics. Dissolution rate of raw QUR was found to be less than 10% in 60 min while in case of QUR loaded LSCs, more than 90% drug release was observed within 5 min. Absence of crystalline peaks of QUR in the DSC and PXRD reports of LSCs and their porous appearance in SEM micrographs indicate that QUR was successfully incorporated in the LSCs. The developed formulation was found to be stable on storage under accelerated stability conditions.
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http://dx.doi.org/10.1016/j.ijbiomac.2021.05.064DOI Listing
July 2021

Sweet pepper and its principle constituent capsiate: functional properties and health benefits.

Crit Rev Food Sci Nutr 2021 May 6:1-25. Epub 2021 May 6.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India.

Capsiate is a non-pungent analogue of capsaicin. It belongs to the family of capsinoids which are esters of vanillyl alcohol with fatty acids while capsaicin belongs to the family of capsaicinoids that are amides of vanillylamine with a variety of branched-chain fatty acids. While capsaicin is extensively reported for plethora of pharmacological actions, capsiate remains much less explored. Extracted from various species of Capsicum plant, the molecule has also been chemically synthesized via a number of synthetic and enzymatic routes. Based on its action on transient receptor potential vanilloid subfamily member 1 receptors, recent research has focused on its potential roles in treatment of obesity, metabolic disorders, cancer, cardiovascular disorders and gastro-intestinal disorders. Its toxicity profile has been reported to be much safe. The molecule, however, faces the challenge of low aqueous solubility and stability. It has been commercialized for its use as a weight loss supplement. However, the therapeutic potential of the compound which is much beyond boosting metabolism remains unexplored hitherto. This comprehensive review summarizes the studies demonstrating the therapeutic potential of capsiate in various pathological conditions. Discussed also are potential future directions for formulation strategies to develop efficient, safe and cost-effective dosage forms of capsiate to explore its role in various disease conditions. The databases investigated include Cochrane library, Medline, Embase, Pubmed and in-house databases. The search terms were "capsiate," "capsinoids," "thermogenesis," and their combinations. The articles were screened for relevance by going through their abstract. All the articles pertaining to physicochemical, physiological, pharmacological and therapeutic effects of capsiate have been included in the manuscript.
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http://dx.doi.org/10.1080/10408398.2021.1913989DOI Listing
May 2021

Harnessing amphiphilic polymeric micelles for diagnostic and therapeutic applications: Breakthroughs and bottlenecks.

J Control Release 2021 06 19;334:64-95. Epub 2021 Apr 19.

Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, Nilgiris, Tamil Nadu, India; Centre of Excellence in Nanoscience & Technology, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, Nilgiris, Tamil Nadu, India.

Amphiphilic block copolymers are widely utilized in the design of formulations owing to their unique physicochemical properties, flexible structures and functional chemistry. Amphiphilic polymeric micelles (APMs) formed from such copolymers have gained attention of the drug delivery scientists in past few decades for enhancing the bioavailability of lipophilic drugs, molecular targeting, sustained release, stimuli-responsive properties, enhanced therapeutic efficacy and reducing drug associated toxicity. Their properties including ease of surface modification, high surface area, small size, and enhanced permeation as well as retention (EPR) effect are mainly responsible for their utilization in the diagnosis and therapy of various diseases. However, some of the challenges associated with their use are premature drug release, low drug loading capacity, scale-up issues and their poor stability that need to be addressed for their wider clinical utility and commercialization. This review describes comprehensively their physicochemical properties, various methods of preparation, limitations followed by approaches employed for the development of optimized APMs, the impact of each preparation technique on the physicochemical properties of the resulting APMs as well as various biomedical applications of APMs. Based on the current scenario of their use in treatment and diagnosis of diseases, the directions in which future studies need to be carried out to explore their full potential are also discussed.
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http://dx.doi.org/10.1016/j.jconrel.2021.04.014DOI Listing
June 2021

Anti-ulcerogenic effect of methanolic extract of Elaeagnus conferta Roxb. seeds in Wistar rats.

J Ethnopharmacol 2021 Jul 20;275:114115. Epub 2021 Apr 20.

Rayat Institute of Pharmacy, Railmajra, SBS Nagar, Punjab, India. Electronic address:

Ethnopharmacological Relevance: Elaeagnus conferta Roxb. (Elaeagnaceae) is a subtropical shrub mainly native to India, Vietnam, Malaysia and South China, whose various parts are used for treatment of diabetes, gastric ulcers, pain, oxidative stress and pulmonary disorders. Though the other parts of the plant have been reported for their ethnic use i.e. fruits as astringent locally and for cancer systemically, leaves for body pain and flowers for pain in chest and the seeds are mentioned as edible, there is no report per se on the medicinal use of seeds. Based on the fact that seeds of closely resembling species i.e. Elaeagnus rhamnoides has demonstrated significant anti-gastroulcerative property, the probability of the seeds of E. conferta possessing similar activity seemed quite significant.

Aim Of The Study: Phytochemical investigation and assessment of pharmacological mechanism(s) involved in anti-ulcer effect of methanolic extract of the seeds of E. conferta.

Materials And Methods: Bioactive phytoconstituents were isolated by column chromatography. These were identified by spectroscopic techniques including infrared (IR) spectroscopy, nuclear magnetic resonance (NMR) and mass spectrometry. Methanolic extract (MEC) of the seeds was prepared by cold maceration and its anti-ulcerogenic potential was evaluated using indomethacin (50 mg/kg) and water immersion stress models in male rats. The animals were pre-treated with different doses of MEC (400 and 800 mg/kg) and the therapeutic effect was compared with standard drug i.e. ranitidine (RANT; 50 mg/kg). The ameliorative effects of MEC were investigated on gastric juice pH, total acidity, free acidity and ulcer index. The assays of malionaldehyde (MDA), catalase (CAT), superoxide dismutase (SOD), glutathione (GSH) and pro-inflammatory cytokines i.e. interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α) were carried out to find out the possible mechanism(s) of protection. Further, histopathological changes were also studied.

Results: Chromatography studies and further confirmation by spectroscopic techniques revealed the presence of four different compounds in MEC i.e oleic acid (1), stearic acid (2), ascorbic acid (3) and quercetin (4). MEC exhibited anti-ulcerogenic effect in dose dependent manner which may be attributed to suppression of pro-inflammatory cytokines (IL-6, TNF-α) and MDA (112.7%), and up-regulation of protective factors such as CAT (90.48%), SOD (92.77%) and GSH (90.01%). Ulcer inhibition, reduction in total and free acidity and increase in gastric juice pH were observed in MEC treated rats as compared to disease control animals. Histopathological findings confirmed decreased cell infiltration, less epithelial cell damage and regeneration of gastric mucosa in dose dependent manner.

Conclusions: The anti-ulcer effect of MEC may be attributed to its ability to scavenge free radicals and anti-inflammatory property via suppression of TNF-α and IL-6, thus offers a complete and holistic approach for management of peptic ulcer.
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http://dx.doi.org/10.1016/j.jep.2021.114115DOI Listing
July 2021

Opening eyes to therapeutic perspectives of bioactive polyphenols and their nanoformulations against diabetic neuropathy and related complications.

Expert Opin Drug Deliv 2021 04 27;18(4):427-448. Epub 2020 Dec 27.

Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, Nilgiris, Tamil Nadu, India.

: Diabetic neuropathy (DN) is one of the major complications arising from hyperglycaemia in diabetic patients. In recent years polyphenols present in plants have gained attention to treat DN. The main advantages associated with them are their action via different molecular pathways to manage DN and their safety. However, they failed to gain clinical attention due to challenges associated with their formulation development such as lipophilicity,poor bioavailability, rapid systemic elimination, and enzymatic degradation.: This article includes different polyphenols that have shown their potential against DN in preclinical studies and the research carried out towards development of their nanoformulations in order to overcome aforementioned issues.: In this review various polyphenol based nanoformulations such as nanospheres, self-nanoemulsifying drug delivery systems, niosomes, electrospun nanofibers, metallic nanoparticles explored exclusively to treat DN are discussed. However, the literature available related to polyphenol based nanoformulations to treat DN is limited. Moreover, these experiments are limited to preclinical studies. Hence, more focus is required towards  development of nanoformulations using simple and single step process as well as inexpensive and non-toxic excipients so that a stable, scalable, reproducible and non-toxic formulation could be achieved and clinical trials could be initiated.
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http://dx.doi.org/10.1080/17425247.2021.1846517DOI Listing
April 2021

Fail-safe nano-formulation of prodrug of sulfapyridine: Preparation and evaluation for treatment of rheumatoid arthritis.

Mater Sci Eng C Mater Biol Appl 2021 Jan 8;118:111332. Epub 2020 Aug 8.

Department of Physiotherapy and Rehabilitation(,) Fortis Hospital, Chandigarh Road, Ludhiana 141015, Punjab, India.

Aim of the present study was to give a second life to the long-abandoned drug, sulfapyridine (SP) for its anti-arthritic potential by design of nano-vesicular delivery system. For this, intra-articular delivery of its liposomal formulation was tried. As the prepared formulation exhibited rapid drug leakage, an arthritis responsive prodrug of SP showing lability towards synovial enzymes was synthesized to exploit the over-expression of arthritis specific enzymes. Prodrug (SP-PD) exhibited better retention in liposomes as compared to the drug, preventing its escape from synovium. Hydrolysis of SP-PD in human plasma and synovial fluid indicated its high susceptibility to enzymes. The liposomes of SP-PD exhibited larger mean size, less PDI and higher zeta potential as compared to those for SP liposomes. In arthritic rats, prodrug liposomes were found to reverse the symptoms of inflammation, including the levels of biochemical markers. Liposomes of bio-responsive prodrug, therefore, offer a revolutionary approach in the treatment of rheumatoid arthritis.
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http://dx.doi.org/10.1016/j.msec.2020.111332DOI Listing
January 2021

Expanding the Arsenal Against Huntington's Disease-Herbal Drugs and Their Nanoformulations.

Curr Neuropharmacol 2021 ;19(7):957-989

Department of Biotechnology, School of Bioengineering and Biosciences, Faculty of Technology and Sciences, Lovely Professional University, Phagwara-144411, Punjab, India.

Huntington's disease (HD) is an autosomal fatal genetic disease in which degeneration of neuronal cells occurs in the central nervous system (CNS). Commonly used therapeutics are cludemonoamine depletors, antipsychotics, antidepressants, and tranquilizers. However, these drugs cannot prevent the psychotic, cognitive, and behavioral dysfunctions associated with HD. In addition to this, their chronic use is limited by their long-term side effects. Herbal drugs offer a plausible alternative to this and have shown substantial therapeutic effects against HD. Moreover, their safety profile is better in terms of side effects. However, due to limited drug solubility and permeability to reach the target site, herbal drugs have not been able to reach the stage of clinical exploration. In recent years, the paradigm of research has been shifted towards the development of herbal drugs based nanoformulations that can enhance their bioavailability and blood-brain barrier permeability. The present review covers the pathophysiology of HD, available biomarkers, phytomedicines explored against HD, ongoing clinical trials on herbal drugs exclusively for treating HD and their nanocarriers, along with their potential neuroprotective effects.
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http://dx.doi.org/10.2174/1570159X18666201109090824DOI Listing
January 2021

Nanocarriers for treatment of dermatological diseases: Principle, perspective and practices.

Eur J Pharmacol 2021 Jan 28;890:173691. Epub 2020 Oct 28.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, Punjab, India.

Skin diseases are the fourth leading non-fatal skin conditions that act as a burden and affect the world economy globally. This condition affects the quality of a patient's life and has a pronounced impact on both their physical and mental state. Treatment of these skin conditions with conventional approaches shows a lack of efficacy, long treatment duration, recurrence of conditions, systemic side effects, etc., due to improper drug delivery. However, these pitfalls can be overcome with the applications of nanomedicine-based approaches that provide efficient site-specific drug delivery at the target site. These nanomedicine-based strategies are evolved as potential treatment opportunities in the form of nanocarriers such as polymeric and lipidic nanocarriers, nanoemulsions along with emerging others viz. carbon nanotubes for dermatological treatment. The current review focuses on challenges faced by the existing conventional treatments along with the topical therapeutic perspective of nanocarriers in treating various skin diseases. A total of 213 articles have been reviewed and the application of different nanocarriers in treating various skin diseases has been explained in detail through case studies of previously published research works. The toxicity related aspects of nanocarriers are also discussed.
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http://dx.doi.org/10.1016/j.ejphar.2020.173691DOI Listing
January 2021

Exploring role of probiotics and Ganoderma lucidum extract powder as solid carriers to solidify liquid self-nanoemulsifying delivery systems loaded with curcumin.

Carbohydr Polym 2020 Dec 29;250:116996. Epub 2020 Aug 29.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, Punjab, India.

Solid self-nanoemulsifying drug delivery system (S-SENDDS) containing Curcumin (CRM) were prepared using combination of Ganoderma lucidum extract powder (GLEP) and probiotics (PB) as carriers. Liquid SNEDDS containing CRM were prepared by mixing Capmul MCM, Labrafil M1944CS, Tween 80 and Transcutol P. These were further spray dried and finally converted into spheroids. The droplet size of reconstituted S-SNEDDS powder and spheroids was found in the range of 35 to 37 nm, zeta potential in the range of - 21.48 to -23.22 mV and drug loading in the range of 95-96%. The release of drug from formulations was found to be more than 90%. Similarly, significant improvement (p < 0.05) in permeability of CRM was observed through SNEDDS using Caco2 cell lines. The non-significant difference (p> 0.05) in drug loading, droplet size, dissolution rate and angle of repose between L-SNEDDS and S-SNEDDS indicated the potential of GLEP-PB to produce stable SNEDDS.
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http://dx.doi.org/10.1016/j.carbpol.2020.116996DOI Listing
December 2020

Fecal Microbiota Transplant: Latest Addition to Arsenal Against Recurrent Clostridium Difficile Infection.

Recent Pat Antiinfect Drug Discov 2020 Sep 24. Epub 2020 Sep 24.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab- 144411. India.

An infectious disease of colon, recurrent Clostridium difficile infection (RCDI) is hitherto considered insurmountable leading to significant morbidity and mortality. Gut dysbiosis, generally resulting from frequent use of antibiotics is considered to be responsible for the etiopathogenesis of rCDI. Ironically, the conventional treatment strategies for the disease also include the use of anti-infective drugs such as metronidazole, vancomycin and fidaxomycin. As a result of the efforts to overcome the limitations of these treatment options to control recurrence of disease, Fecal Microbiota Transplant (FMT) has emerged as an effective and safe alternative. It is pertinent to add here that FMT is defined as the process of engraftment of fecal suspension from the healthy person into the gastrointestinal tract of the diseased individual aiming at the restoration of gut microbiota. FMT has proved to be quite successful in the treatment of recurrent and resistant Clostridium difficile infections (RCDI). In last three decades a lot of information has been generated on the use of FMT for RCDI. A number of clinical trials have been reported with generally very high success rates. However, very small number of patents could be found in the area indicating that there still exists lacuna in the knowledge about FMT with respect to its preparation, regulation, mode of delivery and safety. The current review attempts to dive deeper to discuss the patents available in the area while supporting the information contained therein with the non-patent literature.
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http://dx.doi.org/10.2174/1574891X15666200925092354DOI Listing
September 2020

OUTBREAK of novel corona virus disease (COVID-19): Antecedence and aftermath.

Eur J Pharmacol 2020 Oct 25;884:173381. Epub 2020 Jul 25.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144411, India.

Outbreak of Coronavirus disease 2019 (COVID-19) started in mid of December 2019 and spread very rapidly across the globe within a month of its outbreak. Researchers all across the globe started working to find out its possible treatments. However, most of initiatives taken were based on various hypotheses and till date no successful treatments have been achieved. Some strategies adopted by China where existing antiviral therapy was initially used to treat COVID-19 have not given very successful results. Researchers from Thailand explored the use of combination of anti-influenza drugs such as Oseltamivir, Lopinavir and Ritonavir to treat it. In some cases, combination therapy of antiviral drugs with chloroquine showed better action against COVID-19. Some of the clinical studies showed very good effect of chloroquine and hydroxychloroquine against COVID-19, however, they were not recommended due to serious clinical toxicity. In some cases, use of rho kinase inhibitor, fasudil was found very effective. In some of the countries, antibody-based therapies have proved fairly successful. The use of BCG vaccines came in light; however, they were not found successful due to lack of full-proof mechanistic studies. In Israel as well as in other developed countries, pluristems allogeneic placental expanded cell therapy has been found successful. Some phytochemicals and nutraceuticals have also been explored to treat it. In a recent report, the use of dexamethasone was found very effective in patients suffering from COVID-19. Its effect was most striking among patients on ventilator. The research for vaccines that can prevent the disease is still going on. In light of the dynamic trends, present review focuses on etiopathogenesis, factors associated with spreading of the virus, and possible strategies to treat this deadly infection. In addition, it attempts to compile the recent updates on development of drugs and vaccines for the dreaded disease.
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http://dx.doi.org/10.1016/j.ejphar.2020.173381DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7381902PMC
October 2020

Enhanced oral bioavailability and neuroprotective effect of fisetin through its SNEDDS against rotenone-induced Parkinson's disease rat model.

Food Chem Toxicol 2020 Oct 23;144:111590. Epub 2020 Jul 23.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144411, India.

Fisetin (FS) was reported to have various pharmacological activities. But due to its lower aqueous solubility and oral bioavailability, it is not in much use. As solubility and bioavailability plays and important role in the pharmacological activity, in this research work we tried to improve the oral bioavailability of fisetin. In this research work, we developed self-nanoemulsifying drug delivery system (SNEDDS) of fisetin. Developed SNEDDS were subjected for pharmacokinetic and pharmacodynamics studies against rotenone-induced Parkinson's disease (PD) model in rats. Higher Cmax and area under the curve during pharmacokinetic study indicated that SNEDDS improved the oral bioavailability of FS and also increased the mean residence time of drug in plasma. Results of behavior parameters (locomotor, muscle co-ordination and catalepsy), biochemical estimation (TBARS, nitrite, GSH, SOD and CAT) and ELISA (soluble alfa synuclein, BDNF, TNF-α and IL-6) confirmed the significantly improved (p < 0.05) neuroprotection in rats treated with FS loaded SNEDDS as compared to rats treated with naïve FS. This study suggests that SNEDDS improved the oral bioavailability of FS which further helped in improving its neuroprotective activity in rat model of PD. It further suggests the potential use of FS-SNEDDS in effective management of PD condition.
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http://dx.doi.org/10.1016/j.fct.2020.111590DOI Listing
October 2020

Validated Reverse Phase-High-Performance Liquid Chromatography Method for Estimation of Fisetin in Self-Nanoemulsifying Drug Delivery System.

Assay Drug Dev Technol 2020 Aug/Sep;18(6):274-281. Epub 2020 Jun 29.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India.

Fisetin (FS) is a polyphenolic phytoconstituent reported to have various pharmacological activities such as antioxidant, antiparkinsonian, and antidepressant. An analytical method was developed and validated for the estimation of FS by ultrafast liquid chromatography using C-18 reverse phase column. Acetonitrile and orthophosphoric acid (0.2% v/v) in the ratio of 30:70 v/v was used as mobile phase. Flow rate was set at 1 mL/min. Chromatogram of FS was detected at wavelength of 362 nm. Retention time for FS was found to be 7.06 min. The developed method was found to be linear in the range of 2-10 μg/mL with regression coefficient of 0.9985. The method was validated as per the International Conference on Harmonization (ICH) Q2 (R1) guidelines. The percentage recovery was in the range of 95%-105%, which indicated the accuracy of the method. The percentage relative standard deviation (RSD) was found to be <2%, which indicates the precision of the method. Limit of detection (LOD) and limit of quantification (LOQ) were found to be 0.46 and 1.41 μg/mL, respectively. The developed method was found to be robust as there was no significant change in response with change in flow rate, ratio of mobile phase, and pH. The method was successfully applied for estimation of drug loading and drug release from self-nanoemulsifying drug delivery system (SNEDDS). The % drug loading of FS in prepared liquid SNEDDS formulation was found to be 101.95%. The results of dissolution studies indicated 67.78% FS release in water at the end of 60 min.
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http://dx.doi.org/10.1089/adt.2020.983DOI Listing
September 2021

High-Performance Liquid Chromatography and Liquid Chromatography/Mass Spectrometry Studies on Stress Degradation Behavior of Sulfapyridine and Development of a Validated, Specific, Stability-Indicating HPLC Assay Method.

Assay Drug Dev Technol 2020 04 8;18(3):119-133. Epub 2020 Apr 8.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, India.

The objective of the current investigation was to develop a simple, rapid, and stability-indicating high-performance liquid chromatography method and to study the degradation behavior of sulfapyridine (SP) under different International Conference on Harmonization (ICH)-recommended conditions. The chromatographic method was developed using C (250 × 4.6 mm, 5 μ) column, and mobile phase consisting of acetonitrile-0.1% formic acid (30:70 v/v) at ambient temperature, at a flow rate of 1 mL/min. The elution was monitored at 265 nm using a photodiode array detector. The developed method was subsequently validated as per ICH Q2 (R1) guidelines. The retention time of SP was observed as 4.56 min with the linearity range between 2 to 10 μg/mL. Limit of detection and limit of quantitation for SP were 0.115 and 0.35 μg/mL, respectively. Forced degradation studies were carried out on bulk samples of SP using prescribed acidic, basic, oxidative, thermal, and photolytic conditions. Extent of degradation in 0.1 M hydrochloric acid and under photolytic conditions was found to be 21.56% and 28.57%, respectively. The degradation products formed in stress conditions were identified by liquid chromatography-mass spectrometry (LC-MS). The utility of the method was verified by quantification of SP in different laboratory-made pharmaceutical preparations. The proposed method could be successfully used to quantify SP in different pharmaceutical dosage forms.
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http://dx.doi.org/10.1089/adt.2019.959DOI Listing
April 2020

Gold nanoparticles: New routes across old boundaries.

Adv Colloid Interface Sci 2019 Dec 17;274:102037. Epub 2019 Oct 17.

Department of Pharmacognosy, Faculty of Pharmacy, Ishik University, Erbil, Kurdistan, Iraq.

In recent years, gold nanoparticles have emerged as unique non-invasive drug carriers for targeting drugs to their site of action. Their site specificity has helped in increasing drugs' efficacy at lower dose as well as reduction in their side effects. Moreover, their excellent optical properties and small size offer their utilization as diagnostic tools to diagnose tumors as well as other diseases. This review focuses on various approaches that have been used in last several years for preparation of gold nanoparticles, their characterization techniques and theranostic applications. Their toxicity related aspects are also highlighted. Gold nanoparticles are useful as theranostic agents, owing to their small size, biocompatible nature, size dependent physical, chemical and optical properties etc. However, the challenges associated with these nanoparticles such as scale up, cost, low drug payload, toxicity and stability have been the major impediments in their commercialization. The review looks into all these critical issues and identifies the possibilities to overcome these challenges for successful positioning of metallic nanoparticles in market.
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http://dx.doi.org/10.1016/j.cis.2019.102037DOI Listing
December 2019

Treatment strategies against diabetes: Success so far and challenges ahead.

Eur J Pharmacol 2019 Nov 23;862:172625. Epub 2019 Aug 23.

Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Australia.

The growing disease burden of diabetes mellitus is an important public health concern, affecting over 400 million people globally. This epidemic, if not controlled in time, leads to life threatening complications, compromise in quality of life, and eventually mortality. Over time, many attempts have been made for the effective treatment of diabetes but true success has never been achieved. Pharmacological and non-pharmacological approaches for the treatment of hyperglycaemia have been ever-evolving due to limitations of current therapies. Non pharmacological management which includes diet management and exercise, has been the primary focus for self-management of diabetes. The pharmacological management includes oral antihyperglycaemics, phytoconstituents, and combination products. Advancements such as nanocarrier delivery systems have been made in drug delivery to overcome the challenges such as poor bioavailability associated with conventional dosage forms currently employed in diabetes treatment. In recent years, much emphasis has been given to synbiotics that act on gut microbiota, as an emerging therapy for diabetes. The current review discusses different treatment strategies for diabetes management starting from insulin therapy to synbiotics. The combination of herbal phytoconstituents with synthetic drugs, synthetic drug combinations, novel drug delivery systems for insulin are highlighted. Moreover, the role of gut dysbiosis in diabetes and its treatment by administration of synbiotics in various clinical as well as non clinical studies has been discussed in detail.
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http://dx.doi.org/10.1016/j.ejphar.2019.172625DOI Listing
November 2019

The Why, Where, Who, How, and What of the vesicular delivery systems.

Adv Colloid Interface Sci 2019 Sep 9;271:101985. Epub 2019 Jul 9.

School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road (NH 1), Phagwara, Punjab 144411, India.

Though vesicular delivery systems have been widely explored and reviewed, no comprehensive review exists that covers their development from the inception of the concept to its culmination in the form of regulated marketed formulations. With the advancement of scientific research in the field of nanomedicine, certain category of vesicular delivery systems have successfully reached the global market. Despite extensive research and highly encouraging results in a plethora of pathological conditions in the preclinical studies, translation of these nanomedicines from laboratory to market has been very limited. Aim of this review is to describe comprehensively the various colloidal delivery systems, focusing mainly on their conventional and advanced methods of preparation, different characterization techniques and main success stories of their journey from bench to bedside of the patient. The review also touches the finer nuances of the use of modern formulation approach of DoE (Design of Experiments) in their formulation and the status of regulatory guidelines for the approval of these nanomedicines.
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http://dx.doi.org/10.1016/j.cis.2019.07.006DOI Listing
September 2019

Nanovesicles for Nanomedicine: Theory and Practices.

Methods Mol Biol 2019 ;2000:1-17

Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, India.

Lipid-based nanovesicles such as liposomes, niosomes, and ethosomes are now well recognized as potential candidates for drug delivery and theranostic applications. Some of them have already stepped forward from laboratory to market. The property to entrap lipophilic drugs in their bilayers and hydrophilic drugs in the aqueous milieu makes them a unique carrier for drug delivery. Delivery of drugs/diagnostics to various organs/tissues/cells via nanovesicles is considered to be a topic of long-standing interest with new challenges being posed to formulation scientists with new developments. The key challenge in this context is the physiological and pathological conditions, which make the delivery of drugs extremely difficult at the disease locus and makes their precise delivery ineffective. This chapter gives an insight into the role of novel nanovesicles in the field of drug delivery. We present an overview of the formulation and characterization and role of diverse nanovesicles. A comprehensive update about their application and current as well as potential challenges have also been discussed.
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http://dx.doi.org/10.1007/978-1-4939-9516-5_1DOI Listing
March 2020

A three-pronged formulation approach to improve oral bioavailability and therapeutic efficacy of two lipophilic drugs with gastric lability.

Drug Deliv Transl Res 2019 08;9(4):848-865

Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, India.

The aim of present study was to co-administer curcumin (CRM) liquisolid pellets and coated duloxetine hydrochloride (DXH) pellets in rats to treat neuropathic pain (NP) associated with chronic constriction injury (CCI). To formulate liquisolid pellets of CRM, it was first dissolved in Tween-80 and then adsorbed on the porous surface of MCC PH102 and Syloid XDP that were used as carrier and coating materials, respectively. Central composite design was used to optimize the liquisolid formulation. The results of powder X-ray diffraction studies, differential scanning calorimetry, and scanning electron microscopy showed complete solubility of drug in Tween-80 followed by its complete adsorption on the porous surface of Syloid XDP and MCC PH102. Both DXH and liquisolid CRM powders were converted into pellets using extrusion-spheronization. DXH pellets were further coated with Eudragit S100 to bypass the gastric pH. About 32.31-fold increase in dissolution rate of CRM present in liquisolid formulation was observed as compared to its unprocessed form. Similarly, the dissolution profile in 0.1 N HCl for Eudragit S100-coated DXH showed complete protection of drug for 2 h and complete release after its introduction in buffer medium (0.2 M phosphate buffer pH 6.8). he pharmacokinetic studies carried out on rats revealed 7.3-fold increase in bioavailability of CRM present in liquisolid pellets and 4.1-fold increase in bioavailability of DXH present in coated pellets was observed as compared to their unprocessed pellets. This increase in bioavailability of drugs caused significant amelioration of CCI-induced pain in rats as compared to their unprocessed forms. The histological sections showed better improvement in regeneration of nerve fibers in rats.
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http://dx.doi.org/10.1007/s13346-019-00635-0DOI Listing
August 2019

Novel drug delivery systems for NSAIDs in management of rheumatoid arthritis: An overview.

Biomed Pharmacother 2018 Oct 14;106:1011-1023. Epub 2018 Jul 14.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India. Electronic address:

Rheumatoid arthritis (RA) is a systemic autoimmune disease characterized by chronic joint inflammation which ultimately leads to severe disability and premature mortality. It has a global prevalence of around 1% with the incidence among women being 2-3 times more than in men. The pathogenesis of the disease involves preclinical RA, genetic factors, and environmental factors. The RA has no known cure and the primary aim of treatment remains to attain lowest possible disease activity and recovery if possible. The present review highlights the literature on the different treatment options available for the treatment of RA, their mechanisms of action, side effects, and novel drug delivery systems that are in use for drug administration with the main focus on novel drug delivery systems of non-steroidal anti-inflammatory drugs. Different classes of drugs such as corticosteroids, non-steroidal anti-inflammatory drugs (NSAIDs) and disease modifying anti-rheumatic drugs (DMARDs), and biologics are discussed with examples of most widely used drugs among each class. Conventional drug therapy has many disadvantages like low solubility and permeability, poor bioavailability, degradation by gastrointestinal enzymes, first pass metabolism, food interactions, and toxicity. Novel drug delivery systems like microspheres, nanoparticles, dendrimers, liposomes, and so on are promising tools as they have been successful in overcoming the disadvantages associated with conventional drug delivery system. The present review squares the various novel drug delivery systems that have been explored for administering anti-rheumatic drugs and the advantages associated with these novel drug delivery systems in comparison to conventional drug delivery systems.
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http://dx.doi.org/10.1016/j.biopha.2018.07.027DOI Listing
October 2018

Prodrugs, phospholipids and vesicular delivery - An effective triumvirate of pharmacosomes.

Adv Colloid Interface Sci 2018 Mar 7;253:35-65. Epub 2018 Feb 7.

Department of Pharmaceutical Analysis, National Institute of Pharmaceutical Education and Research, S.A.S. Nagar, Mohali, Punjab, India.

With the advent from the laboratory bench to patient bedside in last five decades, vesicular systems have now come to be widely accepted as pragmatic means for controlled delivery of drugs. Their success stories include those of liposomes, niosomes and even the lately developed ethosomes and transferosomes. Pharmacosomes, which, as delivery systems offer numerous advantages and have been widely researched, however, remain largely unacknowledged as a successful delivery system. Though a large number of drugs have been derivatized and formulated into self-assembled vesicular systems, the term pharmacosomes has not been widely used while reporting them. Therefore, their relative obscurity may be attributed to the non-usage of the nomenclature of pharmacosomes by the researchers working in the area. We present a review on the scenario that lead to origin of these bio-inspired vesicles composed of self-assembling amphiphilic molecules. Various drugs that have been formulated into pharmacosomes, their characterization techniques, their properties relative to those of other vesicular delivery systems, and the success achieved so far are also discussed.
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http://dx.doi.org/10.1016/j.cis.2018.01.003DOI Listing
March 2018

Sub-chronic safety evaluation of aqueous extract of (.) leaves in rats.

J Adv Pharm Technol Res 2017 Jul-Sep;8(3):108-113

Department of Pharmacology, School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India.

Conventionally, the juice and extract of leaves have been used for the treatment of diabetes, wound healing, dog bite, and as a poultice in rheumatism. To carry out the sub-chronic toxicity and thereafter safety evaluation of leaves. The aqueous extract of leaves was administered orally at the doses of 200, 400, and 800 mg/kg/day for 90 days. All the animals were observed daily for general behavior, changes in body weight, food, and water consumption. At the end of the treatment period, biochemical and hematological parameters were analyzed; and the animals were sacrificed for histopathological examination of heart, lungs, liver, and kidney. The general behavior and water intake were normal in all the rats. The increase in body weight was observed in female rats of all the groups while body weight was decreased in high dose group animals of both sexes. Hematological parameters were not disturbed by the continuous use of extract. A significant decrease in glucose level was observed in intermediate- and high-dose group animals while urea and creatinine level were significantly high in animals of high-dose group. Although histopathological examination of most of the organs exhibited no structural changes, some tubal damage in kidneys was observed in high-dose group animals. The high dose of extract has shown mild signs of toxicity on kidney function test, but no toxic response was observed on hematological and liver biochemical parameters. The extract also exhibited hypoglycemic potential.
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http://dx.doi.org/10.4103/japtr.JAPTR_69_17DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5527696PMC
August 2017

Application of liposomes in treatment of rheumatoid arthritis: quo vadis.

ScientificWorldJournal 2014 4;2014:978351. Epub 2014 Feb 4.

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, India.

The most common treatments for rheumatoid arthritis include nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, disease modifying antirheumatic drugs (DMARDs), and some biological agents. However, none of the treatments available is able to achieve the ultimate goal of treatment, that is, drug-free remission. This limitation has shifted the focus of treatment to delivery strategies with an ability to deliver the drugs into the synovial cavity in the proper dosage while mitigating side effects to other tissues. A number of approaches like microemulsions, microspheres, liposomes, microballoons, cocrystals, nanoemulsions, dendrimers, microsponges, and so forth, have been used for intrasynovial delivery of these drugs. Amongst these, liposomes have proven to be very effective for retaining the drug in the synovial cavity by virtue of their size and chemical composition. The fast clearance of intra-synovially administered drugs can be overcome by use of liposomes leading to increased uptake of drugs by the target synovial cells, which in turn reduces the exposure of nontarget sites and eliminates most of the undesirable effects associated with therapy. This review focuses on the use of liposomes in treatment of rheumatoid arthritis and summarizes data relating to the liposome formulations of various drugs. It also discusses emerging trends of this promising technology.
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http://dx.doi.org/10.1155/2014/978351DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3932268PMC
October 2014
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