Formulation of Ketoconazole Loaded Nano Dispersive Gel Using Swollen Micelles Technique and Its in Vitro Characterization

Reza, Mohammad Irshad; Goel, Divya; Gupta, Rahul; Warsi, Musarrat Hussain

doi:10.22159/ijpps.2018v10i3.24552

Cited by 7 publications

(6 citation statements)

References 12 publications

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“…Zeta potential, PDI index, and particle size for each transferosome formula were determined using dynamic light scattering techniques at 25°C using the particle size system, (Zetasizer, Malvern, UK; Beckman Coulter, USA). Transferosomal colloidal dispersions were diluted with pure water before measurement [10].…”

Section: Particle Size Pdi Index and Zeta Potential Measurementsmentioning

confidence: 99%

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

2020

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Objective: The aim of this study was to develop transferosome vesicles for the transdermal drug delivery of lynestrenol.Methods: The lynestrenol transferosome vesicle was made by encapsulating the drug in a variation of phosphatidylcholine and Tween 80 by the thinlayerhydration method. The resulting transferosome vesicles were modified with a time variation of 30, 60, 90, and 120 min, and sonication variationswere paused and not paused. Particle size evaluation, polydispersity (PDI), and entrapment efficiency (%EE) were carried out on the variation ofsonication time.Results: The evaluation results showed that sonication without pauses showed better %EE and particle size than sonication with pauses andincreasing concentration of Tween 80 (edge activator). The %EE increased, and particle size decreased with increasing sonication time; PDI of vesicleswas heterogeneous with increasing sonication time. The %EE in formulas F1 and F2 after 120 min was 73.06% and 76.06% (paused) and 80.40% and82.97% (without paused). The particle size of formula F1 and F2 after 120 min 575.4 nm and 471.6 nm (paused) and 524.1 nm and 434.7 nm (withoutpaused). The PDI formulas of F1 and F2 after 120 min were 0.69 and 0.763 (paused) and 0.84 and 0.59 (without paused).Conclusion: Based on the results of the transferosome vesicle characteristics, it was shown that the optimal vesicle composition for packaginglynestrenol was vesicles that were composed of phosphatidylcholine and Tween 80 without pauses and could potentially be used as a transdermaldrug delivery system.

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Section: Particle Size Pdi Index and Zeta Potential Measurementsmentioning

confidence: 99%

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

2020

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“…poloxamer 407 with formulation codes from GLY-1 to GLY-12. The best formulation had been identified and further subjected to both in vitro and in vivo studies [3][4][5]. The present study brought out the best formulation with an enhanced dissolution and bioavailability.…”

Section: Introductionmentioning

confidence: 85%

Bioavailability and Dissolution Enhancement of Glyburide Nanosuspension

2019

Asian J Pharm Clin Res

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Objective: The main objective was to develop nanosuspension of glyburide (GLY) by quasi emulsification solvent diffusion method and to enhance dissolution and bioavailability characteristics of the drug GLY, an antidiabetic drug which belongs to Biopharmaceutical Classification System-II category. Materials and Methods: In this work, nanoparticles were prepared using polyvinyl alcohol, hydroxypropyl methyl cellulose, and Eudragit RL100. Twelve formulations of GLY (GLY-1–GLY-12) were formulated using the excipients at various compositions. Drug and excipient compatibility studies were conducted using Fourier transform infrared and differential scanning calorimeter. The prepared nanosuspension was analyzed using scanning electron microscopy for surface of the particle analysis, melting point, solubility, particle charge zeta (mv), percentage drug entrapment efficiency (%), and in vitro drug release. The optimized formulations of nanosuspension were further studied for in vivo pharmacokinetic evaluation. Reverse-phase high-performance liquid chromatography method was developed, validated, and used for the study of these formulations in rat plasma. Results: From these studies, it was confirmed that drugs and excipients chosen were compatible with each other. GLY-8 was the best formulation with a particle size of 85–96 nm with 168.7°C melting point, freely soluble in phosphate buffer pH 7.4, 93.53% drug entrapment, and 90.26±1 mV of zeta potential. This formulation shows percentage drug release of 99.85% in 24 h. In vivo pharmacokinetic study for optimized formulation (GLY -8) suggested that there was no reaction with the rat plasma. From the results, it was shown that Cmax and Tmax were found to be 0.604±0.03 μg/ml and 2±1.01 h, respectively. The values of t1/2 (h), area under the curve (AUC) (0-t), and AUC (0-∞) were found to be 10.04 h, 2.562±0.41 μg.h/ml, and 2.147±0.45 μg.h/ml, respectively. Conclusion: Based on the results obtained, oral administration of nanosuspension could not only provide the better absorption of poorly water soluble drugs but may also reduce toxicity and provide a new tool in drug delivery system.

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“…All experiments were performed in triplicate and the mean values were calculated. The percentage cumulative penetration per square centimeter of gel was plotted against time for each formulation [14,15].…”

Section: In Vitro Diffusion Testsmentioning

confidence: 99%

In Vitro Study of a Transfersomal Gel Preparation Containing Lynestrenol as a Transdermal Drug Delivery System

2020

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Objective: Lynestrenol, a progestin hormone derivative, can suppress the productions of endogenous estrogen and progesterone hormones (ovaries)to prevent ovulation. In this study, lynestrenol was included in various transfersomal gel preparations for its transdermal delivery into fat (F)-andnon-fat (NF)-containing skin tissues.Methods: Lynestrenol transfersome vesicles were prepared by encapsulating the drug in varied concentrations of phosphatidylcholine and Tween80 using lipid film hydration method. Transfersomes were produced in the form of gel preparations at a dose of 0.15 mg/week and evaluated fortheir particle size, percentage of entrapment efficiency, and particle polydispersity. We performed in vitro evaluations of the formulation variants F0(lynestrenol gel control) and F1 and F2 (lynestrenol transfersome gels) with variations in their phosphatidylcholine and Tween 80 content. We thenperformed an in vitro evaluation using the Franz diffusion cell (FDC) method for 12 h using all three formulations on F and NF-containing rat skin.Results: The FDC results demonstrated that lynestrenol was deposited into fat tissue and increased concentrations of Tween 80 (edge activator)increased lynestrenol delivery into this tissue. In addition, the percentages of drug penetration from NF rat skin treated with F0, F1, and F2 gels were19.56%, 20.13%, and 20.56%, respectively, and those from F rat skin were 17.16%, 17.38%, and 17.50%, respectively.Conclusion: In vitro evaluation using the FDC method indicates that transdermal drug delivery through to fat tissues using transfersomes is apromising method for lynestrenol delivery.

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Formulation of Ketoconazole Loaded Nano Dispersive Gel Using Swollen Micelles Technique and Its in Vitro Characterization

Cited by 7 publications

References 12 publications

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

Effects of Sonication on Size Distribution and Entrapment of Lynestrenol Transferosome

Bioavailability and Dissolution Enhancement of Glyburide Nanosuspension

In Vitro Study of a Transfersomal Gel Preparation Containing Lynestrenol as a Transdermal Drug Delivery System

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