Microemulsion Based Bioadhesive Gel of Itraconazole Using Tamarind Gum: In-vitro and Ex-vivo Evaluation

Year 2017, Volume: 21 Issue: 3, 688 - 700, 24.06.2017

Kailas K Mali Shashikant C Dhawale Remeth J Dias

https://doi.org/10.12991/marupj.323593

Abstract

The current study was aimed to formulate and evaluate

bioadhesive gel containing microemulsion (ME) of itraconazole

(ITZ) and an attempt was made to investigate suitability of

tamarind gum (TG) as a gelling agent. The solubility of ITZ

in oils, surfactants and co-surfactant was evaluated for the

selection of appropriate component. The ratio of surfactant and

co-surfactant was optimized by constructing pseudoternary

phase diagram. Ternary phase diagram was constructed using

isopropyl myristate (IPM) and oleic acid (OA) as oil phase, tween

80 as surfactant and isopropyl alcohol (IPA) as cosurfactant

in order to obtain ME region. The optimized ME of ITZ was

characterized by its qualitative and quantitative tests and

incorporated into polymeric gels of carbopol (CBP), xanthan

gum (XG) and TG. The ME based ITZ gels were evaluated for

pH, drug content, viscosity, ex-vivo bioadhesion, spreadability

and in vitro drug release. Furthermore, antifungal activity of

the gels was performed by agar cup diffusion technique using

cultures of Candida albicans. ITZ showed maximum solubility

in mixture of IPM and OA (1:1). Stable ME was obtained when

IPM and OA was taken in the ratio of 1:1 as oil phase, Tween 80

as surfactant and isopropyl alcohol (IPA) as cosurfactant at the

weight ratio of 10:45:45. The optimized ME based gels showed

pH in the range of 6.11 to 6.48, spreadability in the range of 4.1

to 7.1gm.cm/sec and ex vivo bioadhesion in the range of 65 to

84gm. The viscosity study indicated pseudoplastic behaviour of

all ME based gel formulations. Amongst the studied ME gels,

TG containing gels exhibited fast and complete drug release at

the end of 24h. Formulation F7 containing TG showed wide

zone of inhibition and found to be stable for three months.

These results indicate that the TG containing ME gel may be a

used as vehicle for topical delivery of drugs.

Keywords

bioadhesion, itraconazole, microemulsion gel, tamarind gum, xanthan gum

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