Publications by authors named "Ameeduzzafar Zafar"

20 Publications

  • Page 1 of 1

Formulation of Chitosan-Coated Piperine NLCs: Optimization, In Vitro Characterization, and In Vivo Preclinical Assessment.

AAPS PharmSciTech 2021 Aug 31;22(7):231. Epub 2021 Aug 31.

Department of Clinical Laboratories Sciences, College of Applied Medical Sciences, Jouf University, Sakaka, Aljouf Region, Saudi Arabia.

In the present research work, surface-modified nanostructured lipid carriers (NLCs) with chitosan (CH) were prepared to improve the therapeutic efficacy of piperine (PP). NLCs were developed and optimized (CH-PP-NLCs-opt) by design expert software and the selected NLCs surface was coated with chitosan (0.2% w/v). CH-PP-NLCs-opt have shown a particle size of 149.34 ± 4.54 nm and entrapment efficiency of 80.65 ± 1.23%. The results of the solid-state characterization study exhibited that PP enclosed in lipids and present amorphous form. It might be due to the nanoparticle size of NLCs. The drug release study revealed PP-NLCs-opt and CH-PP-NLCs-opt exhibited significant (P < 0.05) difference in PP release (88.87 ± 5.23% and 76.34 ± 4.54%) as compared to pure PP (19.02 ± 2.87%). CH-PP-NLCs-opt exhibited strong bioadhesion than PP-NLCs-opt which has a positive influence the drug permeation and absorption. CH-PP-NLCs-opt showed higher permeation (1083.34 ± 34.15 μg/ cm2) than pure PP (106.65 ± 15.44 μg/cm) and PP-NLCs-opt (732.45 ± 28.56 μg/ cm). The significantly enhanced bioavailability of PP was observed from CH-PP-NLCs-opt (3.76- and 1.21-fold) than PP-dispersion and PP-NLCs-opt. The diabetes was induced in rats by a single intraperitoneal administration of streptozotocin (STZ, 40 mg/kg, citrate buffer pH 4.5), and results revealed that PP-NLCs-opt and CH-PP-NLCs-opt reduce the blood glucose level (28.26% and 36.52% respectively) as compared to PP-dispersion (10.87%). It also helps to maintain the altered biochemical parameters. In conclusion, CH-PP-NLC can be a novel oral nanocarrier for the management of diabetes.
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http://dx.doi.org/10.1208/s12249-021-02098-4DOI Listing
August 2021

Exploring indole-based-thiadiazole derivatives as potent acetylcholinesterase and butyrylcholinesterase enzyme inhibitors.

Int J Biol Macromol 2021 Oct 11;188:1025-1036. Epub 2021 Aug 11.

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, Saudi Arabia.

Indole based thiadiazole derivatives (1-18) were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition. The IC values of the synthesized analogues ranging between 0.17 ± 0.05 to 33.10 ± 0.6 μM against (AChE) and 0.30 ± 0.1 to 37.60 ± 0.6 μM against (BChE) enzymes. Among the series compounds 8 (IC = 0.17 ± 0.05 μM) (IC = 0.30 ± 0.1 μM), 9 (IC = 0.30 ± 0.05 μM) (IC = 0.60 ± 0.05 μM) and 10 (IC = 1.30 ± 0.1 μM) (IC = 2.60 ± 0.1) were found to be the most potent analogues bearing para, ortho, and meta-fluoro substitutions on phenyl ring attached to thiadiazole. In addition, all the synthesized scaffolds were characterized by using H NMR, C NMR spectroscopy, and high-resolution Mass Spectrometry (HR-MS). To apprehend the binding mode of interaction of the most potent synthesized derivatives, a molecular docking study was performed.
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http://dx.doi.org/10.1016/j.ijbiomac.2021.08.065DOI Listing
October 2021

Formulation and Optimization of Butenafine-Loaded Topical Nano Lipid Carrier-Based Gel: Characterization, Irritation Study, and Anti-Fungal Activity.

Pharmaceutics 2021 Jul 16;13(7). Epub 2021 Jul 16.

Department of Pharmacy, College of Health Sciences, Arsi University, Asella P.O. Box 396, Ethiopia.

The present study aims to prepare and optimize butenafine hydrochloride NLCs formulation using solid and liquid lipid. The optimized selected BF-NLCopt was further converted into Carbopol-based gel for topical application for the treatment of fungal infection. Box Behnken design was employed to optimize the nanostructure lipids carriers (NLCs) using the lipid content (A), Tween 80 (B), and homogenization cycle (C) as formulation factors at three levels. Their effects were observed on the particle size (Y) and entrapment efficiency (Y). The selected formulation was converted into gel and further assessed for gel characterization, drug release, anti-fungal study, irritation study, and stability study. The solid lipid (Compritol 888 ATO), liquid lipid (Labrasol), and surfactant (tween 80) were selected based on maximum solubility. The optimization result showed a particle size of 111 nm with high entrapment efficiency of 86.35% for BF-NLCopt. The optimized BF-NLCopt converted to gel (1% /, Carbopol 934) and showed ideal gel evaluation results (drug content 99.45 ± 2.11, pH 6.5 ± 0.2, viscosity 519 ± 1.43 CPs). The drug release study result depicted a prolonged drug release (65.09 ± 4.37%) with high drug permeation 641.37 ± 46.59 µg (32.07 ± 2.32%) than BF conventional gel. The low value of irritation score (0.17) exhibited negligible irritation on the skin after application. The anti-fungal result showed greater efficacy than the BF gel at both time points. The overall conclusion of the results revealed NLCs-based gel of BF as an ideal delivery system to treat the fungal infection.
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http://dx.doi.org/10.3390/pharmaceutics13071087DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8309199PMC
July 2021

Formulation of carteolol chitosomes for ocular delivery: formulation optimization, permeation, and ocular toxicity examination.

Cutan Ocul Toxicol 2021 Aug 3:1-12. Epub 2021 Aug 3.

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

:Conventional delivery systems like solution and suspension are commonly used for the treatment of ocular diseases but have low corneal residence time and hence the duration of effect is limited. These drawbacks of conventional systems can be reduced by preparing bioadhesive chitosan (CH) coated noisome.: Niosomes (NIM) of carteolol (CT) were developed by the thin-film hydration method and optimised by the Box-Behnken statistical design. Further, the optimised CT-NIM was coated with CH to enhance the ocular residence time . The optimised formulation was evaluated for vesicle size, entrapment efficiency, and drug release and transcorneal permeation, histopathology, etc.: CT-NIM-opt showed the vesicle size and entrapment efficiency of 235 ± 3.54 nm, and 70.45 ± 0.87%, respectively. DSC spectra exhibited that CT was completely encapsulated into the CH-CT-NIM matrix. Drug release from CH-CT-NIM-opt was more sustained (68.28 ± 4.2%) than CT-NIM (75.69 ± 4.5% in 12 h) and CT solution (99.89 ± 2.8% in 4 h). The CH-CT-NIM-opt represented a strong bio-adhesion (89.76 ± 3.6%) than CT-NIM-opt (15.65 ± 3.4%). The permeation flux exhibited 1.13-fold higher permeation than CT-NIM and 3.23 fold than CT solution. The corneal hydration was found to be within the limit value. The histopathology study exhibited no structural damage to the cornea . HET-CAM results showed zero scores indicating no bleeding or haemorrhage. CH-CT-NIM-opt was found to be isotonic and exhibited good stability when stored at 4 °C for the stated duration of time.: The above findings suggested that NIM can be a potential carrier for the delivery of CT with better ocular residence time.
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http://dx.doi.org/10.1080/15569527.2021.1958225DOI Listing
August 2021

6-Shogaol attenuated ethylene glycol and aluminium chloride induced urolithiasis and renal injuries in rodents.

Saudi J Biol Sci 2021 Jun 14;28(6):3418-3423. Epub 2021 Mar 14.

Department of Pharmaceutics, College of Pharmacy, Jouf University, Aljouf 72341, Saudi Arabia.

The 6-shogaol, is a flavanone type flavonoid that is abundant in citrus fruit and has a wide range of pharmacological effects. The present study attempted to evaluate the antiurolithic effect of 6-shogaol on ethylene glycol (EG) and ammonium chloride (AC)-induced experimental urolithiasis in rats. The efficacy of 6-shogaol 50 mg/kg and 100 mg/kg was studied in EG 0.75% (V/V) and AC 1% (W/V) experimentally induced urolithiasis in rats for 21 days. The weight difference, urine volume, the levels of calcium, phosphate, magnesium, oxalate and uric acid in urine was observed. The blood urea nitrogen, creatinine, uric acid in serum and levels of malondialdehyde (MDA) and glutathione (GSH) were also measured. Histopathological analyses in kidneys were also performed. The rats weights were higher in the 6-shogaol groups than the urolithiasis group. EG caused a significant increase in serum creatinine (p < 0.05), BUN (P < 0.001), and uric acid (p < 0.01) while treatment with Cystone (750 mg/kg), and 6-shogaol (50 and 100 mg/kg) showed the significant reduction in increased serum levels of creatinine (p < 0.001), uric acid (p < 0.01) and BUN (p < 0.001). Administration of EG and AC showed statistically significant (p < 0.001) elevated levels of MDA and reduction in GSH levels. Treatment of Cystone (750 mg/kg), and 6-shogaol (50 and 100 mg/kg) significantly (p < 0.001) reduced MDA levels and an increase GSH levels as compared to EG and AC-treated group. The histological findings further attested antiurolithiatic properties of 6-shogaol. The present study attributed clinical shreds of evidence first time that claiming the significant antiurolithic effect of 6-shogaol and could be a cost-effective candidate for the prevention and treatment of urolithiasis.
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http://dx.doi.org/10.1016/j.sjbs.2021.03.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8176042PMC
June 2021

Formulation of Piperine-Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation.

Molecules 2021 May 29;26(11). Epub 2021 May 29.

Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi Arabia.

The present research work is designed to prepare and evaluate piperine liposomes and piperine-chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (-7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly ( < 0.001)) reduced the IC when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.
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http://dx.doi.org/10.3390/molecules26113281DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8198173PMC
May 2021

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment.

Saudi Pharm J 2021 Mar 22;29(3):269-279. Epub 2021 Feb 22.

Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City, Cairo, Egypt.

Aim: Diabetic (type-2) is a metabolic disease characterized by increased blood glucose level from the normal level. In the present study, apigenin (AG) loaded lipid vesicles (bilosomes: BIL) was prepared, optimized and evaluated for the oral therapeutic efficacy.

Experimental: AG-BIL was prepared by a thin-film evaporation method using cholesterol, span 60 and sodium deoxycholate. The prepared formulation was optimized by 3-factor and 3-level Box-Behnken design using particle size, entrapment efficiency and drug release as a response. The selected formulation further evaluated for  permeation,  pharmacokinetic and pharmacodynamics study.

Results: The optimized AG bilosomes (AG-BILopt) has shown the vesicle size 183.25 ± 2.43 nm, entrapment efficiency 81.67 ± 4.87%. TEM image showed a spherical shape vesicle with sharp boundaries. The drug release study revealed a significant enhancement in AG release (79.45 ± 4.18%) from AG-BILopt as compared to free AG-dispersion (25.47 ± 3.64%). The permeation and pharmacokinetic studies result revealed 4.49 times higher flux and 4.67 folds higher AUC than free AG-dispersion. The antidiabetic activity results showed significant (P < 0.05) enhancement in therapeutic efficacy than free AG-dispersion. The results also showed marked improvement in biochemical parameters.

Conclusion: Our findings suggested, the prepared apigenin loaded bilosomes was found to be an efficient delivery in the therapeutic efficacy in diabetes.
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http://dx.doi.org/10.1016/j.jsps.2021.02.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8085606PMC
March 2021

Methanolic extract of Cucumis melo attenuates ethylene glycol-induced nephrolithiasis in Wistar rats.

Urolithiasis 2021 Aug 9;49(4):301-308. Epub 2021 Apr 9.

Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.

Evaluation of the effects of methanolic extract of Cucumis melo in ethylene glycol-induced nephrolithiasis on Wistar rats. 0.75% solution of ethylene glycol (EG) in payable water was given to produce nephrolithiasis on Wistar rats. The action of oral intake of methanolic extract of Cucumis melo seed in nephrolithiasis is studied and is matched with the action of oral intake of Cystone (standard) on Wistar rats. EG resulted in hyperoxaluria and deposition of calcium oxalate as well as raised urinary excretion of oxalate and calcium. Supplementation with methanolic extract of Cucumis melo seed decreased the increased renal oxalate, indicating a regulatory effect on oxalate formation endogenously. The outcomes stipulate that the seed of Cucumis melo is endowed with antinephrolithiatic action.
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http://dx.doi.org/10.1007/s00240-021-01263-5DOI Listing
August 2021

Antibiotic-Loaded Psyllium Husk Hemicellulose and Gelatin-Based Polymeric Films for Wound Dressing Application.

Pharmaceutics 2021 Feb 7;13(2). Epub 2021 Feb 7.

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Aljouf 72388, Saudi Arabia.

Wound infections are one of the major reasons for the delay in the healing of chronic wounds and can be overcome by developing effective wound dressings capable of absorbing exudate, providing local antibiotic release, and improving patient comfort. Arabinoxylan (AX) is a major hemicellulose present in psyllium seed husk (PSH) and exhibits promising characteristics for developing film dressings. Herein, AX-gelatin (GL) films were prepared by blending AX, gelatin (GL), glycerol, and gentamicin (antibiotic). Initially, the optimal quantities of AX, GL, and glycerol for preparing transparent, bubble-free, smooth, and foldable AX-GL films were found. Physiochemical, thermal, morphological, drug release, and antibacterial characteristics of the AX-GL films were evaluated to investigate their suitability as wound dressings. The findings suggested that the mechanical, water vapor transmission, morphological, and expansion characteristics of the optimized AX-GL films were within the required range for wound dressing. The results of Fourier-transform infrared (FTIR) analyses suggested chemical compatibility among the ingredients of the films. In in vitro drug release and antibacterial activity experiments, gentamicin (GM)-loaded AX-GL films released approximately 89% of the GM in 24 h and exhibited better antibacterial activity than standard GM solution. These results suggest that AX-GL films could serve as a promising dressing to protect against wound infections.
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http://dx.doi.org/10.3390/pharmaceutics13020236DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7914473PMC
February 2021

Development and machine-learning optimization of mucoadhesive nanostructured lipid carriers loaded with fluconazole for treatment of oral candidiasis.

Drug Dev Ind Pharm 2021 Feb 8;47(2):246-258. Epub 2021 Jan 8.

Faculty of Pharmacy, Department of Pharmaceutics and Industrial Pharmacy, Beni-Suef University, Beni-Suef, Egypt.

The aim of this work was to prepare and optimize mucoadhesive nanostructured lipid carrier (NLC) impregnated with fluconazole for better management of oral candidiasis. The NLCs were fabricated using an emulsification/sonication technique. The nanoparticles consisted of stearic acid, oleic acid, Pluronic F127, and lecithin. Box-Behnken design, artificial neural networking, and variable weight desirability were employed to optimize the joint effect of drug concentration in the drug/lipid mixture, solid lipid concentration in the solid/liquid lipid mixture, and surfactant concentration in the total mixture on size and entrapment. The optimized NLCs were coated with chitosan. The nanoparticles were characterized by surface charge, spectroscopic, thermal, morphological, mucoadhesion, release, histopathological, and antifungal properties. The nanoparticles are characterized by a particle size of 335 ± 13.5 nm, entrapment efficiency of 73.1 ± 4.9%, sustained release, minor histopathological effects on rabbit oral mucosa, and higher fungal inhibition efficiency for an extended period of time compared with fluconazole solution. Coating the nanoparticles with chitosan increased its adhesion to rabbit oral buccal mucosa and improved its anti-candidiasis activity. It is concluded that mucoadhesive lipid-based nanoparticles amplify the effect of fluconazole on . This finding warrants pre-clinical and clinical studies in oral candidiasis disease models to corroborate findings.
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http://dx.doi.org/10.1080/03639045.2020.1871005DOI Listing
February 2021

Enhanced full-thickness wound healing via extract delivery based on a chitosan/gelatin dressing incorporating microemulsion.

Drug Dev Ind Pharm 2021 Feb 4;47(2):215-224. Epub 2021 Jan 4.

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi Arabia.

There are many synthetic drugs in literature have been utilized in healing of the wounds although the natural product specially antioxidants can offer similar if not better biological activity in that regard. Genus Sophora is well known to contain flavonoids and phenolic compounds which have antioxidant and inflammatory effects. So, the aim of the current study was to develop and evaluate chitosan/gelatin based extract-loaded microemulsion as wound dressing. extract (SGE) contained 16 major compounds which have reasonable antioxidant activity. The developed microemulsion showed that Tween 80 produced significant ( < 0.05) lower particle size than Pluronic F127 at the same SGE concentration whereas high concentration of extract results in large particle size. Thermodynamic stability studies showed that using higher concentration of the extract produced less stable formulations. The selected formulation was impregnated in the dressing base (chitosan/gelatin; 2:1 w/w ratio) which exhibited more water absorption. evaluation revealed that the dressing displayed superior wound repair compared to the control in terms histological examination and determination of alpha smooth muscle actin (α-SMA) and proliferating cell nuclear antigen (PCNA). Thus, SGE-loaded microemulsion-impregnated gelatin/chitosan could be a potential candidate for the wound healing.
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http://dx.doi.org/10.1080/03639045.2020.1863420DOI Listing
February 2021

Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, in vitro Characterization and ex vivo Intestinal Permeation Study.

J Oleo Sci 2020 ;69(11):1389-1401

Department of Pharmaceutics, College of Pharmacy, Jouf University.

The oral route is the most prevalent route of drug administration among various routes. Dapagliflozin is an oral hypoglycemic drug used for lowering the blood glucose level. The objective of this work is to developed and optimized dapagliflozin loaded nanostructured lipid carriers (DG-NLCs) for the improvement of oral delivery. DG-NLCs were prepared by a high-pressure homogenization method (hot) and optimized by Box-Behnken design software using lipid, surfactant, and homogenization cycle as an independent variable. DG-NLCs were evaluated for particle size (Y), entrapment efficiency (Y), drug release (Y). The DG-NLCs were further evaluated for morphology, thermal and X-ray diffraction analysis, ex-vivo intestinal permeation, and stability study. Particle size (nm), entrapment efficiency (%) and drug release (%) of all seventeen formulations were found in the range of 113.71-356.22 nm, 60.43-96.54% and 63.44-83.62% respectively. Morphology of optimized formulation exhibited spherical in shape confirmed by transmission electron microscopy. Thermal and X-ray diffraction analysis of NLCs showed the drug was solubilized and lost the crystallinity. DG-NLCs-opt exhibited dual release pattern initial fast and later sustained-release (90.01±2.01% in 24 h) whereas DG-dispersion showed 31.54±1.87% release in 24 h. Korsmeyer-Peppas model was found to be the best fit model (R=0.999). The DG-NLCs-opt exhibited significant-high (p < 0.05, 1.293 µg/cm/h) flux than DG-dispersion (0.2683 µg/cm/h). Apparent permeation coefficient of DG-NLCs-opt was found to be significantly higher (p < 0.05, 4.14×10 cm/min) than DG-dispersion (8.61×10 cm/min). The formulation showed no significant changes (p < 0.05) on six months of storage study at 25±2°C/60±5%RH. The finding concluded that quality by design (QbD) based lipid nanocarrier for oral delivery could be a promising approach of dapagliflozin for the management of diabetes.
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http://dx.doi.org/10.5650/jos.ess20162DOI Listing
November 2020

Clarithromycin-Loaded Ocular Chitosan Nanoparticle: Formulation, Optimization, Characterization, Ocular Irritation, and Antimicrobial Activity.

Int J Nanomedicine 2020 13;15:7861-7875. Epub 2020 Oct 13.

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Purpose: The topically administered drugs through conventional delivery systems have low bioavailability. Henceforth, the present study was designed to prepare and optimize clarithromycin (CTM)-loaded chitosan nanoparticles (CHNPs) to demonstrate the efficacy against microorganisms.

Methods: Clarithromycin-loaded chitosan nanoparticles (CTM-CHNPs) were prepared by ionotropic gelation method. The formulation was optimized by box-Behnken design using the formulation variables like CH (A), STPP concentration (B), and stirring speed (C). Their effects were evaluated on the independent variables like particle size (Y) and entrapment efficiency (Y). Further, CTM-CHNPs were evaluated for physicochemical parameters, in-vitro drug release, ex-vivo permeation, bioadhesive study, corneal hydration, histopathology, HET-CAM, and antibacterial study.

Results: The optimized formulation (CTM-CHNPopt) showed the low particle size (152±5 nm), which is desirable for ocular delivery. It also showed high encapsulation (70.05%), zeta potential (+35.2 mV), and was found in a spherical shape. The drug release study revealed a sustained drug release profile (82.98±3.5% in 12 hours) with Korsmeyer peppas kinetic (R=0.996) release model. It showed a 2.7-fold higher corneal permeation than CTM-solution. CHNPs did not exhibit any sign of damage to excised goat cornea, which is confirmed by hydration, histopathology, and HET-CAM test. It exhibited significant (<0.05) higher antibacterial susceptibility than CTM-solution.

Conclusion: The finding of the study concluded that CTM-CHNPs can be used for effective management of bacterial conjunctivitis by increasing the precorneal residence time.
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http://dx.doi.org/10.2147/IJN.S269004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7568680PMC
November 2020

Formulation of amorphous ternary solid dispersions of dapagliflozin using PEG 6000 and Poloxamer 188: solid-state characterization, study, and molecular simulation assessment.

Drug Dev Ind Pharm 2020 Sep 5;46(9):1458-1467. Epub 2020 Aug 5.

Department of Pharmacy Practice, Unaizah College of Pharmacy, Qassim University, Buraydah, Saudi Arabia.

The present study was designed to prepare dapagliflozin (DFG) loaded ternary solid dispersions (SDs) using the carrier blend polyethylene glycol 6000 (PEG 6000) and poloxamer 188 (PLX 188). The prepared DFG-SDs were evaluated for solubility study, physicochemical characterization and molecular simulation study. The prepared DFG-SDs showed significant higher solubility and dissolution vis-a-vis pure DFG and DFG physical mixture. The composition DFG:PEG:PLX (1:2.25:0.75 mM) showed the highest solubility (0.476 ± 0.016 mg/mL). The physicochemical characterization confirms the polymorphic transition of DFG from crystalline state to stable amorphous form. The prepared DFG-SDs showed a significantly higher dissolution (64.78 ± 2.34% to 78.41 ± 2.39%) than pure DFG (15.70 ± 3.54%). DFG-SD2 showed a significantly enhanced drug permeation (<.05) (58.76 ± 4.65 µg/cm) as compared to pure DFG (14.97 ± 3.32 µg/cm). The molecular docking study result revealed a good hydrophobic interaction of DFG with the used carrier due to the lowest energy pose. The interaction occurs between the methylene bridges and the central hydrophobic chain of polyoxypropylene of the polymer. Therefore, DFG-SDs prepared by microwave irradiation method using hydrophilic carrier blend might be a promising strategy for improving the solubility and dissolution performance.
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http://dx.doi.org/10.1080/03639045.2020.1802482DOI Listing
September 2020

Stimulus Responsive Ocular Gentamycin-Ferrying Chitosan Nanoparticles Hydrogel: Formulation Optimization, Ocular Safety and Antibacterial Assessment.

Int J Nanomedicine 2020 30;15:4717-4737. Epub 2020 Jun 30.

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Al-Jouf, Kingdom of Saudi Arabia.

Purpose: The present study was designed to study the gentamycin (GTM)-loaded stimulus-responsive chitosan nanoparticles to treat bacterial conjunctivitis.

Methods: GTM-loaded chitosan nanoparticles (GTM-CHNPs) were prepared by ionotropic gelation method and further optimized by 3-factor and 3-level Box-Behnken design. Chitosan (A), sodium tripolyphosphate (B), and stirring speed (C) were selected as independent variables. Their effects were observed on particle size (PS as Y1), entrapment efficiency (EE as Y2), and loading capacity (LC as Y3).

Results: The optimized formulation showed the particle size, entrapment efficiency, and loading capacity of 135.2±3.24 nm, 60.18±1.65%, and 34.19±1.17%, respectively. The optimized gentamycin-loaded chitosan nanoparticle (GTM-CHNPopt) was further converted to the stimulus-responsive sol-gel system (using pH-sensitive carbopol 974P). GTM-CHNPopt sol-gel (NSG5) exhibited good gelling strength and sustained release (58.99±1.28% in 12h). The corneal hydration and histopathology of excised goat cornea revealed safe to the cornea. It also exhibited significant (p<0.05) higher ZOI than the marketed eye drop.

Conclusion: The finding suggests that GTM-CHNP-based sol-gel is suitable for ocular delivery to enhance the corneal contact time and improved patient compliance.
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http://dx.doi.org/10.2147/IJN.S254763DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7335305PMC
August 2020

Nano Phytomedicine Based Delivery System for CNS Disease.

Curr Drug Metab 2020 ;21(9):661-673

Department of Pharmaceutics, College of Pharmacy, University of Hafr Al Batin, Al Jamiah, Hafr Al Batin- 39524, Saudi Arabia.

Herbal medicines are being used since ancient times and are an important part of the alternative and traditional medicinal system. In recent decades, scientists are embracing herbal medicines based on the fact that a number of drugs that are currently in use are derived directly or indirectly from plant sources. Moreover, herbal drugs have lesser side effects, albeit are potentially strong therapeutic agents. The herbal medicine market is estimated to be around US $62 billion globally. Herbal medicine has gained widespread acceptance due to its low toxicity, low cost, ease of accessibility and efficacy in treating difficult diseases. Safety and efficacy are another important factors in the commercialization process of herbal medicines. Nanotechnology has been shown to be potentially effective in improving the bioactivity and bioavailability of herbal medicines. Development of nano-phytomedicines (or by reducing the size of phytomedicine), attaching polymers with phytomedicines and modifying the surface properties of herbal drugs, have increased the solubility, permeability and eventually the bioavailability of herbal formulations. Novel formulations such as niosomes, liposomes, nanospheres, phytosomes etc., can be exploited in this area. This article reviews herbal medicines, which have prominent activity in the Central Nervous System (CNS) disorders and reported nano-phytomedicines based delivery systems.
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http://dx.doi.org/10.2174/1389200221666200523161003DOI Listing
January 2020

Long-Acting Paliperidone Parenteral Formulations Based on Polycaprolactone Nanoparticles; the Influence of Stabilizer and Chitosan on In Vitro Release, Protein Adsorption, and Cytotoxicity.

Pharmaceutics 2020 Feb 16;12(2). Epub 2020 Feb 16.

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakakah P.O. Box 2014, Saudi Arabia.

Long-acting preparations containing the antipsychotic paliperidone for intramuscular injection has drawn considerable attention to achieve harmless long-term treatment. This study aimed to develop paliperidone loaded polycaprolactone (PCL) nanoparticles and investigate the influence of PCL/drug ratio, stabilizer type, and chitosan coating on physicochemical properties, protein adsorption, and cellular toxicity. Results showed that chitosan coating produced enlarged particle sizes, shifted the surface charges from negative into positive and did not influence encapsulation efficiencies. Chitosan coating relatively sustained the drug release especially in pluronic stabilized formulations. Pluronic F127 based formulations exhibited the least protein adsorption (384.3 μg/mL). Chitosan coating of Tween 80 and polyvinyl alcohol stabilized formulations significantly ( < 0.05) increased protein adsorption. Cellular viability was concentration-dependent and negatively affected by stabilizers. All formulations did not show cellular death at 1.56 μg/mL. Inflammatory responses and oxidative stress were less affected by Tween 80 compared with other stabilizers. Chitosan minimized all aspects of cellular toxicity. Collectively, stabilizer type and chitosan coating play critical roles in developing safe and effective long-acting PCL nanoparticles intended for parenteral drug delivery. The coated formulations containing Tween 80 and Pluronic F127 as stabilizers are warranted a future in vivo study to delineate its safety and efficacy profiles.
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http://dx.doi.org/10.3390/pharmaceutics12020160DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076490PMC
February 2020

Optimisation of ethosomal nanogel for topical nano-CUR and sulphoraphane delivery in effective skin cancer therapy.

J Microencapsul 2020 Mar 18;37(2):91-108. Epub 2019 Dec 18.

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.

The optimisation and evaluation of ethosomal nanogel (NGs) for topical delivery in skin cancer. The formulations were optimised by employing 3-factor, 3-level Box Behnken design for responses of vesicle size, and fluxes. They characterised and evaluated for drug release, permeation and retention, skin penetration of ethosome, electron microscopy, texture analysis, and cytotoxicity. The optimised formulation exhibited z-average 125.67 ± 10.43 nm, apparent zeta potential -17.1 ± 2.61 mV, average flux of drug loaded ethosome were 54.72 ± 5.45 and 59.83 ± 6.09 µg/cm/h. Further, Rhodamine B loaded ethosome penetrated deeper up to 183.82 µm. The NGs texture analysis showed index of viscosity 225.45 g.s, firmness 209.34 g, cohesiveness -189.48 g, and consistency 59.45 g.s. The optimised ethosome NGs exhibited significant anti-cancer effect in B16-F10 murine tumour cell line ( < 0.05). Ethosomal NGs could be promising for skin cancer treatment.
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http://dx.doi.org/10.1080/02652048.2019.1701114DOI Listing
March 2020

Intranasal delivery of mucoadhesive nanocarriers: a viable option for Parkinson's disease treatment?

Expert Opin Drug Deliv 2019 12 8;16(12):1355-1366. Epub 2019 Nov 8.

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.

: Intranasal drug delivery is a largely unexplored, promising approach for the treatment of various neurological disorders. However, due to the challenging constraints available in the pathway of nose-to-brain delivery, finding an effective treatment for Parkinsonism is still an impending mission for research workers. This warrants development of novel treatment alternatives for Parkinson's disease (PD). Intranasal delivery of mucoadhesive nanocarriers is one such novel approach which might help in curbing the glitches associated with the currently available therapy.: This review summarizes the evidences supporting nose-to-brain delivery of polymer-based mucoadhesive nanocarriers for the treatment of PD. A concise insight into the lipid-based mucoadhesive nanocarriers has also been presented. The recent researches have been compiled pertaining to the use of mucoadhesive nanocarrriers for improving the treatment outcomes of PD via intranasal drug delivery.: Although the use of nanocarrier-based strategies for site-specific delivery via intranasal route has proven effective, the magnitude of improvement remains moderate resulting in limited translation from industry to the market. Comprehensive understanding of the mucoadhesive polymer, its characteristics and mechanisms involved for an effective nose-to-brain uptake of the drug is a promising avenue to develop novel formulations for effective management of Parkinson disease.
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http://dx.doi.org/10.1080/17425247.2019.1684895DOI Listing
December 2019

Soy isoflavone-loaded alginate microspheres in thermosensitive gel base: attempts to improve wound-healing efficacy.

J Pharm Pharmacol 2019 May 14;71(5):774-787. Epub 2019 Jan 14.

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi Arabia.

Objectives: This study aims to develop thermosensitive gel containing soy isoflavone (antioxidant and anti-inflammatory natural agent) alginate microspheres for enhancement of wound-healing performance.

Methods: Soy isoflavone microspheres were prepared by ionic cross-linking method and optimized using the Box-Behnken optimization design. Formulations were characterized in terms of particle size, encapsulation efficiency and equilibrium swelling degree. The optimized formula was incorporated in Pluronic F127 gel base and examined for in vivo wound-healing efficacy.

Key Findings: Results showed mean particle size between 18 and 25 μm, encapsulation efficiency of over 75% and equilibrium swelling degree over 1.9. Thermal analysis indicated interaction between alginate and CaCl and embedding of soy isoflavone in microspheres. In vivo wound-healing efficacy showed significant advance in re-epithelization, mature collagen synthesis and proangiogenesis. Immunohistochemical investigation exhibited promising alpha-smooth muscle actin immunopositive cells expression, fibroblast activation and expression of proliferating cell nuclear antigen (proliferation marker) in the epidermis and in the dermis.

Conclusions: The developed formulation would appear to be a promising topical preparation for accelerating healing process.
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http://dx.doi.org/10.1111/jphp.13066DOI Listing
May 2019
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