Abstract

Objective: Nanostructured lipid carrier (NLC)-based topical gel of lornoxicam (LXM) was formulated with the aim of controlled release action and to reduce systemic side effect for the treatment of an arthritic condition.
 Methods: NLCs developed using high-pressure homogenization method and optimized using a 32 factorial design with response surface methodology using design expert software. NLCs were characterized for particle size, zeta potential analysis, drug entrapment efficiency, and in vitro drug release studies to select the optimized formulation. The NLCs were suitably gelled and evaluated with respect to homogeneity, pH, viscosity, gel strength, spreadability, rheological characteristics, drug content, in vitro diffusion, and stability study. Safety of the NLC-based gel was assessed using primary skin irritation studies, and efficacy was confirmed using carrageenan-induced rat paw edema model.
 Results: NLCs formulation comprising 2% of lipid (60:40) and surfactant (1.50%) was confirmed as an optimized batch having a particle size (138.2±3.60 nm) with polydispersibility index value 0.344±0.034. The zeta potential value indicates good physical stability. Based on the results from the in vitro release study it was shown that the formed gels had the ability to extend release of LXM for 24 h and showing percentage drug release of 90.92%±1.96% at the end of 24 h. Skin irritation studies revealed that the optimized gel formulation shows no erythema, edema, or ulceration.
 Conclusion: The overall results of the present study clearly indicated promising potentials of NLC-based gel for delivering LXM topically over the conventional gel.

Highlights

  • In the past decade, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) have been looked on as promising carriers for presenting several attractive features for transdermal drug delivery [1]

  • Selection of lipids Based on the screening of lipids, for the maximum solubility of the drug in Precirol was selected as solid lipid for the formulation of NLC’s and has property such as good flow property, non toxicity, approved regulatory status, and cost which favors its choice as solid lipid, oleic acid was screened out as most suitable liquid lipid to be used in the LXM-NLCs and poloxamer 188 was selected as a surfactant phase for the formulation of NLCs

  • Drug-excipients interaction study The possible interaction between the drug and the ingredients used in the preparation of the NLC was studied by FTIR and differential scanning calorimetry (DSC)

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Summary

Introduction

Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) have been looked on as promising carriers for presenting several attractive features for transdermal drug delivery [1]. These carriers are composed of physiological and biodegradable lipids exhibiting low systemic toxicity and low cytotoxicity. The small size of the lipid particles ensures close contact with stratum corneum and can increase the amount of drug penetrating into mucosa or skin Due to their solid lipid matrix, a controlled release from these carriers is possible [1,2]. NLCs are the new generation of lipid nanoparticles, attracting major attention as novel colloidal drug carriers for topical use [4,5]

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