Investigation of microemulsion system for transdermal delivery of itraconazole

Chudasama, Arpan; Patel, Vineetkumar; Nivsarkar, Manish; Vasu, Kamala K.; Shishoo, C. J.

doi:10.4103/2231-4040.79802

Cited by 45 publications

(12 citation statements)

References 32 publications

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“…The spindle number 2 was dipped in microemulsion and rotated at 5, 10, 20, and 50 rpm at room temperature. [23] For the viscosity of hydrogel, the spindle number 6 was dipped in the preparation and rotated at 5, 10, 20, and 50 rpm at room temperature. The viscosity of microemulsion-based hydrogel was determined by using Brookfield viscometer.…”

Section: Methodsmentioning

confidence: 99%

Formulation and evaluation of microemulsion-based hydrogel for topical delivery

Sabale

Vora

2012

Int J Pharma Investig

127

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Background:The purpose of this study was to develop microemulsion-based hydrogel formulation for topical delivery of bifonazole with an objective to increase the solubility and skin permeability of the drug.Materials and Methods:Oleic acid was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems. The pseudo-ternary phase diagrams for microemulsion regions were constructed using oleic acid as the oil, Tween 80 as the surfactant and isopropyl alcohol (IPA) as the cosurfactant. Various microemulsion formulations were prepared and optimized by 32 factorial design on the basis of percentage (%) transmittance, globule size, zeta potential, drug release, and skin permeability. The abilities of various microemulsions to deliver bifonazole through the skin were evaluated ex vivo using Franz diffusion cells fitted with rat skins. The Hydroxy Propyl Methyl Cellulose (HPMC) K100 M as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The optimized microemulsion-based hydrogel was evaluated for viscosity, spreadability, skin irritancy, skin permeability, stability, and antifungal activity by comparing it with marketed bifonazole cream.Results:The mechanism of drug release from microemulsion-based hydrogel was observed to follow zero order kinetics. The studied optimized microemulsion-based hydrogel showed a good stability over the period of 3 months. Average globule size of optimized microemulsion (F5) was found to be 18.98 nm, zeta potential was found to be -5.56 mv, and permeability of drug from microemulsion within 8 h was observed 84%. The antifungal activity of microemulsion-based hydrogel was found to be comparable with marketed cream.Conclusion:The results indicate that the studied microemulsion-based hydrogel (F5) has a potential for sustained action of drug release and it may act as promising vehicle for topical delivery of ibuprofen.

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Section: Methodsmentioning

confidence: 99%

Formulation and evaluation of microemulsion-based hydrogel for topical delivery

Sabale

Vora

2012

Int J Pharma Investig

127

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“…Flux divided by donor concentration resulted in apparent permeability coefficient (K p ). [13] Mean and standard deviation were calculated using Microsoft Excel 2003. The experiments were performed in triplicate ( n = 3) and data was subjected to one-way ANOVA at a significance level of P ≤ 0.05 using MINITAB 16 software (Minitab Inc., PA, USA).…”

Section: Methodsmentioning

confidence: 99%

Terpenes: Effect of lipophilicity in enhancing transdermal delivery of alfuzosin hydrochloride

Prasanthi

Lakshmi

2012

J Adv Pharm Tech Res

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Transdermal drug delivery has attracted much attention as an alternative to intravenous and oral methods of delivery. But the main barrier is stratum corneum. Terpenes classes of chemical enhancers are used in transdermal formulations for facilitating penetration of drugs. The aim of the study is to evaluate terpenes as skin penetration enhancers and correlate its relationship with permeation and lipophilicity. In this study, alfuzosin hydrochloride (AH) hydrogels were prepared with terpenes using Taguchi orthogonal array experimental design. The formulations contained one of eight terpenes, based on their lipophilicity (log P 2.13-5.36). The percutaneous permeation was studied in rat skin using diffusion cell technique. Flux, cumulative amount, lag time and skin content of AH were measured over 24 hours and compared with control gels. Nerolidol with highest lipophilicity (log P 5.36 ± 0.38) showed highest cumulative amount (Q24) of 647.29 ± 18.76 μg/cm2 and fluxrateof 28.16 ± 0.64 μg/cm2/hour. It showed decreased lag time of 0.76 ± 0.15 hours. Fenchone (2.5%) (log P 2.13 ± 0.30) produced the longest lag time 4.8 ± 0.20 hours. The rank order of enhancement effect was shown as nerolidol > farnesol > limonene > linalool > geraniol > carvone > fenchone > menthol. Lowest skin content was seen with carvone. Increase in lipophilicity of terpenes showed increase in flux, cumulative amount (Q24), and enhancement ratio which was significant with P < 0.000. But lag time was decreased and no correlation was found between lipophilicity and skin content. Histological studies showed changes in dermis which can be attributed to disruption of lipid packing of stratum corneum due to effect of nerolidol within lipid lamellae. It was found that small alcoholic terpenes with high degree of unsaturation enhance permeation of hydrophilic drugs, liquid terpenes enhance better than solid terpenes and terpenes with high lipophilicity are good penetration enhancers.

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“…Microemulsions enhance the bioavailability of poorly soluble antiviral and antiretroviral drugs such as acyclovir, penciclovir, ritonavir by maintaining them in molecular dispersion in the GI tract and hence, extend the absorption window available in the GI lumen. [ 12 13 ]…”

Section: Formulation Approaches Of Antiviral and Antiretroviral Agentmentioning

confidence: 99%

Novel drug delivery approaches on antiviral and antiretroviral agents

Sharma

Chawla

Arora

et al. 2012

J Adv Pharm Tech Res

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Viruses have the property to replicate very fast in host cell. It can attack any part of host cell. Therefore, the clinical efficacy of antiviral drugs and its bioavailability is more important concern taken into account to treat viral infections. The oral and parenteral routes of drug administration have several shortcomings, however, which could lead to the search for formulating better delivery systems. Now, a day's novel drug delivery systems (NDDS) proved to be a better approach to enhance the effectiveness of the antivirals and improve the patient compliance and decrease the adverse effect. The NDDS have reduced the dosing frequency and shorten the duration of treatment, thus, which could lead the treatment more cost-effective. The development of NDDS for antiviral and antiretroviral therapy aims to deliver the drug devoid of toxicity, with high compatibility and biodegradability, targeting the drug to specific sites for viral infection and in some instances it also avoid the first pass metabolism effect. This article aims to discuss the usefulness of novel delivery approaches of antiviral agents such as niosomes, microspheres, microemulsions, nanoparticles that are used in the treatment of various Herpes viruses and in human immunodeficiency virus (HIV) infections.

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Investigation of microemulsion system for transdermal delivery of itraconazole

Cited by 45 publications

References 32 publications

Formulation and evaluation of microemulsion-based hydrogel for topical delivery

Formulation and evaluation of microemulsion-based hydrogel for topical delivery

Terpenes: Effect of lipophilicity in enhancing transdermal delivery of alfuzosin hydrochloride

Novel drug delivery approaches on antiviral and antiretroviral agents

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