Central composite design-based optimization, formulation and characterization of tretinoin-loaded lipoidal cubic-shaped nanocarriers

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Shailja, Neha Jain, Amit Chaudhary, Upendra Nagaich

Abstract

Lipoidal cubic-shaped nanocarriers or cubosomes are self-assembling, nanoscale cubic structures used to regulate the release of therapeutic moieties from their lipoidal matrix. The half-life of tretinoin, a potent anti-acne agent is 0.5-2h. The challenge with tretinoin on its topical application is irritation, redness, and enhanced photosensitivity when applied directly on the skin. The aim of the current work is to formulate tretinoin-loaded cubosomes with minimum particle size, maximum entrapment and sustained release with an intention to reduce the above-mentioned challenges. Seventeen formulations were developed using central composite design with three independent variables i.e., glyceryl monooleate, poloxamer 407, and stirring speed at two different levels. Based on desirability function, optimized formulation was developed and characterized for particle size, entrapment efficiency, zeta potential, and in vitro drug release. The results of optimized formulation with reference to particle size, zeta potential, and entrapment efficiency were 176.2 nm, -20.3 mV, and 70.8% ± 0.29 respectively. The in vitro drug release study depicted a release of 83.39% ± 1.96 at the end of 24 h. These studies demonstrated that the cubosomes can be a potential nanocarrier for the delivery of photosensitive drug with sustained release.

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