Publications by authors named "Vilasrao J Kadam"

12 Publications

  • Page 1 of 1

BCS class II drug loaded protein nanoparticles with enhanced oral bioavailability: evaluation and pharmacokinetic study in rats.

Drug Dev Ind Pharm 2020 Jun 15;46(6):955-962. Epub 2020 May 15.

Bharati Vidyapeeth's College of Pharmacy, Navi Mumbai, India.

The aim of the study was to improve the bioavailability of atorvastatin calcium (ATC) by formulating polymeric nanoparticles (NPs) with an easy and cost-effective approach. ATC entrapped gelatin nanoparticles (AEGNPs) were prepared by using a simple one-step desolvation method. The formed NPs were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, and differential scanning calorimetry. Morphological study exhibited a homogenous spherical shape of formulated NPs. FTIR studies revealed the chemical compatibility of the drug with gelatin. The improvement in drug delivery kinetics of AEGNPs could be attributed to amorphization along with the reduction in particle size of ATC. The pharmacokinetic study in Sprague-Dawley rats revealed that the and AUC of AEGNPs in rats were ∼4-fold and ∼11-fold higher than that of pure ATC suspension. The research presented successfully shows that AEGNPs preparation by one-step desolvation, using minimum excipients is a quick, easy and reproducible method. These results suggest that the ATC encapsulated gelatin NP is a promising approach for the oral delivery of ATC, improving the bioavailability of the drug.
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http://dx.doi.org/10.1080/03639045.2020.1764021DOI Listing
June 2020

Graphene: A Comprehensive Review.

Curr Drug Targets 2017 ;18(6):724-733

Bharati Vidyapeeth's College of Pharmacy, CBD Belapur, Navi Mumbai, Maharashtra, 400614, India.

Graphene, a one-atom thick, two-dimensional sheets of sp2hybridized carbon atoms packed in a hexagonal lattice with a Caron-Carbon distance of about 0.142 nm. Its extended honeycomb network forms the basic building block of other important allotropes; it can be stacked to form 3-Dgraphite, rolled to form 1-D-nanotubes and wrapped to form 0-D-fullerenes. Long-range π conjugation in graphene results in its extraordinary thermal, mechanical and electrical properties, which have been the interest of many theoretical studies and recently became an exciting area for scientists. Graphene is impermeable to gas and liquids, has excellent thermal conductivity and higher current density in comparison to other most effective materials. All of its exceptional properties have opened up new avenues for the use of graphene in nano-devices and nano-systems, which initiated its prominent use as a material for drug targeting. In addition, several fabrication techniques are outlined, starting from the mechanical exfoliation of high-quality graphene to the direct growth on silicon carbide or metal substrates and from the chemical routes utilizing graphene oxide to the newly developed approach at the molecular level. By this article reviewers intend to emphasize on unique properties, fabrication techniques and updated applications of graphene. In addition, we discuss about the potential of graphene in drug targeting in fields of nanotechnology, biomedical engineering and technology and its use for innovations in various fields such as electronics and photonics.
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http://dx.doi.org/10.2174/1389450117666160709023425DOI Listing
April 2018

Chitosan: a propitious biopolymer for drug delivery.

Curr Drug Deliv 2015 ;12(4):369-81

University of Mumbai, Bharati Vidyapeeth's College of Pharmacy, Department of Quality Assurance, CBD Belapur, Sector-8, Navi-Mumbai-400614, India.

Scientists have always been interested in the use of natural polymers for drug delivery. Chitosan, being a natural cationic polysaccharide has received a great deal of attention in the past few years. It is obtained by deacetylation of chitin and is regarded as the second most ubiquitous polymer subsequent to cellulose on earth. Unlike other natural polymers, the cationic charge possessed by chitosan is accountable for imparting interesting physical and chemical properties. Chitosan has been widely exploited for its mucoadhesive character, permeation enhancing properties and controlled release of drugs. Moreover it's non-toxic, biocompatible and biodegradable properties make it a good candidate for novel drug delivery system. This review provides an insight on various chitosan based formulations for drug delivery. Some of the current applications of chitosan in areas like ophthalmic, nasal, buccal, sublingual, gastro-retentive, pulmonary, transdermal, colon-specific and vaginal drug delivery have been discussed. In addition, active targeting of drugs to tumor cells using chitosan has been described. Lastly a brief section covering the safety aspects of chitosan has also been reviewed.
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http://dx.doi.org/10.2174/1567201812666150310151657DOI Listing
May 2016

Cubosomes: Innovative Nanostructures for Drug Delivery.

Curr Drug Deliv 2016 ;13(4):482-93

University of Mumbai, Bharati Vidyapeeth's College of Pharmacy, Department of Pharmaceutics, CBD Belapur, Sector-8, Navi-Mumbai-400614, India.

Background: Some amphiphilic lipids can self-assemble to form bicontinuous cubic liquid crystalline materials in aqueous media. These cubic structures have gained considerable attention since they impart unique properties of practical interest. Cubosomes, being dispersions of an inverted type bicontinuous cubic phase, separate two continuous aqueous regions with a lipid bilayer having the propensity to incorporate drugs of varying polar characteristics. These novel versatile materials possess the properties to form a section of the next generation of advanced biocompatible nanoparticles.

Methods: This review chiefly considers the scope and importance of cubosomes as a proficient drug delivery vehicle. In addition, it also takes into account the various methods of preparation, the drug loading and release behavior as well as different methods of characterization. Their current advances in various arenas ranging from sustained drug release, burn management, melanoma therapy, vaccine delivery, protein delivery, cosmeceutical and theranostic applications are briefly summarized in this overview.

Results: The drug release from cubosomal dispersions have shown enhancement in bioavailability by solubilisation of poorly water soluble drugs, decrease in adverse effects, enhancement of intracellular penetration, protection against degradation, possibility of sustained drug release and the biodegradable nature of lipids is an added advantage.

Conclusion: Recognizing the desirable properties of cubosomes, it has been proposed as a novel carrier for drug delivery systems. Their unique solubilizing, encapsulating, transporting and protecting capabilities make them an attractive vehicle for numerous in vivo drug delivery routes.
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http://dx.doi.org/10.2174/1567201812666150224114751DOI Listing
February 2017

Nanodiamonds as a new horizon for pharmaceutical and biomedical applications.

Curr Drug Deliv 2015 ;12(3):271-81

University of Mumbai, Bharati Vidyapeeth's College of Pharmacy, Department of Pharmaceutics, CBD Belapur, Sector-8, Navi-Mumbai-400614, India.

A palpable need for the optimization of therapeutic agents, due to challenges tackled by them such as poor pharmacokinetics and chemoresistance, has steered the journey towards novel interdisciplinary scientific field for emergence of nanostructure materials as a carrier for targeted delivery of therapeutic agents. Amongst various nanostructures, nanodiamonds are rapidly rising as promising nanostructures that are suited especially for various biomedical and imaging applications. Advantage of being biocompatible and ease of surface functionalization for targeting purpose, besides safety which are vacant by nanodiamonds made them a striking nanotool compared to other nonmaterials which seldom offer advantages of both functionality as well as safety. This review outlines the summary of nanodiamonds, regarding their types, methods of preparation, and surface modification. It also portrays the potential applications of nanodiamond as targeted drug delivery of various bioactive agents. Based on photoluminescent and optical property, nanodiamonds are envisioned as an efficient bioimaging nanostructure. Nanodiamonds as a novel platform hold great promise for targeting cancer cells and in-vivo cell imaging. Based upon their inimitable properties and applications nanodiamonds propose an exciting future in field of therapeutics and thus possess vibrant opportunities.
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http://dx.doi.org/10.2174/1567201812666141229104304DOI Listing
February 2016

Cyclodextrin-based nanosponges: a propitious platform for enhancing drug delivery.

Expert Opin Drug Deliv 2014 Jan 4;11(1):111-20. Epub 2013 Dec 4.

University of Mumbai, Bharati Vidyapeeth's College of Pharmacy, Department of Pharmaceutics , Sector 8, C B D Belapur, Navi Mumbai 400 614 , India +91 022 27571122 ; +91 022 27574525 ;

Introduction: Recently, Nanotechnology is receiving considerable acknowledgment due to its potential to combine features that are difficult to achieve by making use of a drug alone. Cyclodextrin-based nanosponges are yet another contemporary approach for highlighting the advancements which could be brought about in a drug delivery system. Statistical analyses have shown that around 40% of currently marketed drugs and about 90% of drugs in their developmental phase encounter solubility-related problems. Cyclodextrin-based nanosponges have the capacity to emerge as a productive approach over conventional cyclodextrins by overcoming the disadvantages associated with the latter.

Areas Covered: This review is intended to give an insight regarding cyclodextrin-based nanosponges such as their physical and chemical properties. In addition, methods of preparation and characterization are discussed along with biocompatibility, and how these nanomeric elements can be exploited in developing effective drug formulations.

Expert Opinion: This emerging technology of cyclodextrin-based nanosponges is expected to provide technical solutions to the formulation arena and to come up with some successful products in the pharmaceutical market. It also has an exciting future in the field of therapeutics wherein it can cater site-directed drug delivery and hence it possesses vibrant opportunities.
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http://dx.doi.org/10.1517/17425247.2014.865013DOI Listing
January 2014

Aptamer-dendrimer bioconjugate: a nanotool for therapeutics, diagnosis, and imaging.

Expert Opin Drug Deliv 2012 Oct 16;9(10):1273-88. Epub 2012 Aug 16.

University of Mumbai, Bharati Vidyapeeth's College of Pharmacy, Department of Pharmaceutics, CBD Belapur, Sector-8, Navi-Mumbai-400614, India.

Introduction: Aptamers hold great promise as molecular tool in biomedical applications due to the therapeutic utility exhibited by their target specificity and sensitivity. Although current development of aptamer is hindered by its probable in vivo degradation, inefficient immobilization on probe surface, and generation of low detection signal, bioconjugation with nanomaterials can feasibly solve these problems. Nanostructures such as dendrimers, with multivalency and nonimmunogenicity, bioconjugated with aptamers have opened newer vistas for better pharmaceutical applications of aptamers.

Areas Covered: This review covers brief overview of aptamers and dendrimers, with specific focus on recent progresses of aptamer-dendrimer (Apt-D) bioconjugate in areas of targeted drug delivery, diagnosis, and molecular imaging along with the discussion on the currently available conjugates, using their in vitro and in vivo results.

Expert Opinion: The novel Apt-D bioconjugates have led to advances in targeting cancer cell, have amplified biosensing, and offered in vivo cell imaging. Because of the unique properties and applications, Apt-D bioconjugate propose an exciting future. However, further research in synthesis of new target-specific aptamers and their conjugation with dendrimers is required to establish full potential of Apt-D bioconjugate.
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http://dx.doi.org/10.1517/17425247.2012.716421DOI Listing
October 2012

Antioxidant and hypolipidemic activity of Kumbhajatu in hypercholesterolemic rats.

Int J Ayurveda Res 2010 Jul;1(3):159-62

Department of Pharmacology, Bharati Vidyapeeth's College of Pharmacy, CBD, Belapur, Navi Mumbai, India.

Objective: To study the efficacy of Kumbhajatu in reducing the cholesterol levels and as an antioxidant in hypercholesterolemic rats.

Materials And Methods: Hypercholesterolemia was induced in normal rats by including 2% w/w cholesterol, 1% w/w sodium cholate and 2.5% w/w coconut oil in the normal diet. Powdered form of Kumbhajatu was administered as feed supplement at 250 and 500 mg/kg dose levels to the hypercholesterolemic rats. Plasma lipid profile, hepatic superoxide dismutase (SOD) activity, catalase activity, reduced glutathione and extent of lipid peroxidation in the form of malondialdehyde were estimated using standard methods.

Results: Feed supplementation with 250 and 500 mg/kg of Kumbhajatu resulted in a significant decline in plasma lipid profiles. The feed supplementation increased the concentration of catalase, SOD, glutathione and HDL-c significantly in both the experimental groups (250 and 500 mg/kg). On the other hand, the concentration of malondialdehyde, cholesterol, triglycerides, LDL-c and VLDL in these groups (250 and 500 mg/kg) were decreased significantly.

Conclusion: The present study demonstrates that addition of Kumbhajatu powder at 250 and 500 mg/kg level as a feed supplement reduces the plasma lipid levels and also decreases lipid peroxidation.
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http://dx.doi.org/10.4103/0974-7788.72487DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2996573PMC
July 2010

Buccal drug delivery of pravastatin sodium.

AAPS PharmSciTech 2010 Mar 19;11(1):416-24. Epub 2010 Mar 19.

Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, C.B.D. Belapur, Navi Mumbai, 400614 Maharashtra, India.

The purpose of this study was to develop and optimize formulations of mucoadhesive bilayered buccal tablets of pravastatin sodium using carrageenan gum as the base matrix. The tablets were prepared by direct compression method. Polyvinyl pyrrolidone (PVP) K 30, Pluronic(R) F 127, and magnesium oxide were used to improve tablet properties. Magnesium stearate, talc, and lactose were used to aid the compression of tablets. The tablets were found to have good appearance, uniform thickness, diameter, weight, pH, and drug content. A 2(3) full factorial design was employed to study the effect of independent variables viz. levels of carrageenan gum, Pluronic F 127 and PVP K30, which significantly influenced characteristics like in vitro mucoadhesive strength, in vitro drug release, swelling index, and in vitro residence time. The tablet was coated with an impermeable backing layer of ethyl cellulose to ensure unidirectional drug release. Different penetration enhancers were tried to improve the permeation of pravastatin sodium through buccal mucosa. Formulation containing 1% sodium lauryl sulfate showed good permeation of pravastatin sodium through mucosa. Histopathological studies revealed no buccal mucosal damage. It can be concluded that buccal route can be one of the alternatives available for the administration of pravastatin sodium.
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http://dx.doi.org/10.1208/s12249-010-9381-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2850451PMC
March 2010

Studies on the effect of water-soluble polymers on drug-cyclodextrin complex solubility.

AAPS PharmSciTech 2009 27;10(3):858-63. Epub 2009 Jun 27.

Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, Sec-8, CBD Belapur, Navi Mumbai 400 614, Maharashtra, India.

The effect of complexation of irbesartan (IRB), a practically water-insoluble drug, with cyclodextrins in presence of different concentrations of water-soluble polymers (PEG 4000 and PVP K-90) on the dissolution rate of the drug has been investigated. Phase solubility studies were carried out to evaluate the solubilizing power of betaCD in association with water-soluble polymers towards IRB and to determine the apparent stability constant (K (S)) of the complexes. Improvement in K(S) value for ternary complexes (IRB-betaCD-polymers) clearly proved the benefit on the addition of water-soluble polymer to increase complexation efficiency. The dissolution rate of the drug from ternary systems containing PEG 4000 and PVP K-90 was higher as compared to the binary system. An optimum increase in the dissolution rate of the drug was observed at a polymer concentration of 5% w/w for PVP K-90 and 10% w/w for PEG 4000. DSC, FTIR, SEM, and XRD studies were carried out to characterize the complexes.
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http://dx.doi.org/10.1208/s12249-009-9274-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2802171PMC
February 2010

Formulation and evaluation of lecithin organogel for topical delivery of fluconazole.

Curr Drug Deliv 2009 Apr;6(2):174-83

Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, CBD Belapur, Sector-8, Navi- Mumbai - 400 614, India.

The purpose of the present study was to develop and investigate the suitability of microemulsion based lecithin organogel formulations for topical delivery of fluconazole in order to bypass its gastrointestinal adverse effects. The ternary phase diagrams were developed and various organogel formulations were prepared using pharmaceutically acceptable surfactant (lecithin) and ethyl oleate (EO). Solubility of fluconazole in EO and EO-lecithin reverse micellar system was determined. The transdermal permeability of fluconazole from different concentrations of lecithin organogels containing EO as oil phase was analyzed using Keshary-Chien diffusion cell through excised rat skin. Solubility of fluconazole in EO-lecithin reverse micellar system was almost 3 folds higher than that in EO. Gelation and immobilization of oil require critical solubility-insolubility balance of gelator. The occurrence of gel phase was lecithin concentration dependent and was observed in 10-60% w/v of system. Organogel containing 300 mM of lecithin showed the higher drug release and better relative consistency. Hence, it was selected for antifungal activity. The increase in antifungal activity of fluconazole in lecithin organogel may be because of the surfactant action of the lecithin and EO that may help in the diffusion of drug. The histopathological data showed that EO-lecithin organogels were safe enough for the topical purpose. Hence, the present lecithin based organogel appears beneficial for topical delivery of fluconazole in terms of easy preparation, safety, stability and low cost.
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http://dx.doi.org/10.2174/156720109787846252DOI Listing
April 2009

Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem hydrochloride.

AAPS PharmSciTech 2007 Sep 7;8(3):E73. Epub 2007 Sep 7.

Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, C.B.D., Navi Mumbai 400 614, Maharashtra, India.

The purpose of this research was to prepare a floating drug delivery system of diltiazem hydrochloride (DTZ). Floating matrix tablets of DTZ were developed to prolong gastric residence time and increase its bioavailability. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to diminished efficacy of the administered dose. The tablets were prepared by direct compression technique, using polymers such as hydroxypropylmethylcellulose (HPMC, Methocel K100M CR), Compritol 888 ATO, alone or in combination and other standard excipients. Sodium bicarbonate was incorporated as a gas-generating agent. The effects of sodium bicarbonate and succinic acid on drug release profile and floating properties were investigated. A 3(2) factorial design was applied to systematically optimize the drug release profile. The amounts of Methocel K100M CR (X1) and Compritol 888 ATO (X2) were selected as independent variables. The time required for 50% (t50) and 85% (t85) drug dissolution were selected as dependent variables. The results of factorial design indicated that a high level of both Methocel K100M CR (X1) and Compritol 888 ATO (X2) favors the preparation of floating controlled release of DTZ tablets. Comparable release profiles between the commercial product and the designed system were obtained. The linear regression analysis and model fitting showed that all these formulations followed Korsmeyer and Peppas model, which had a higher value of correlation coefficient (r). While tablet hardness had little or no effect on the release kinetics and was found to be a determining factor with regards to the buoyancy of the tablets.
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http://dx.doi.org/10.1208/pt0803073DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2750569PMC
September 2007