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

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 (Y1) and entrapment efficiency (Y2). 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% w/v, 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.

SOME MULTIFUNCTIONAL LIPID EXCIPIENTS AND THEIR PHARMACEUTICAL APPLICATIONS

This review is generally focussed on lipid-based excipients in solid oral formulations which increase its bioavailability. Several approaches have been used to deliver the drug efficiently in the body, and lipid excipients are one of the promising drug delivery systems which address challenges like solubility and bioavailability of water-soluble drugs. Lipids excipients can be tailored to meet a wide range of product requirements like disease indication, route of administration, stability, toxicity, and efficacy. This review discusses novel lipids like Compritol 888 ATO, Dynasan 114, and Precirol ATO 5 and how these can be employed for devicing efficient drug delivery models and thereby have used in cosmetic and pharmaceutical industries.

IDENTIFICATION OF KEY VARIABLES AFFECTIN G DRUG RELEASE FROM LIPID MATRIX IN HYDROALCOHOLIC DISSOLUTION MEDIUM CONTAININ G HYDROXYPROPYL METHYLCELLULOSE

The present research work was undertaken to formulate modified release tablets of lornoxicam using Compritol 888 ATO as a lipid matrixing agent and to evaluate the tablets for dissolution in hydro-alcoholic dissolution media to meet the requirement of regulators. The dissolution study was also conducted in aqueous medium containing alcohol and hydroxylpropyl methylcellulose to mimic the viscosity and pH after food and alcohol intake. The tablets were prepared by direct compression by adopting the concept of design of experiments and evaluated mainly for dissolution studies in aqueous dissolution media containing 10, 25 and 40% ethyl alcohol. The formulated tablets satisfied the USP requirements of drug release at 2, 6 and 10 hr. The drug release was insignificantly altered when the dissolution study was conducted in media containing increasing amount of alcohol probably due to higher solubility of the drug in alcohol. The drug release was suppressed when HPMC was used in the dissolution media. This may be due to rise in viscosity of the dissolution media. Dose dumping was not noticed under the experimental conditions.