Statistical optimization and physicochemical characterization of acitretin-loaded nanostructured lipid carriers for enhanced topical delivery and sustained drug release

Abhishek Kumar Gautam*, Vikash Gupta, Atul Kumar

Ravishankar College of Pharmacy, Bhopal, Madhya Pradesh, India

Refer this article

Abhishek Kumar Gautam, Vikash Gupta, Atul Kumar, 2026. Statistical optimization and physicochemical characterization of acitretin-loaded nanostructured lipid carriers for enhanced topical delivery and sustained drug release. Journal of medical pharmaceutical and allied sciences, V 15, I 3, Pages 22 – 28. Doi: https://doi.org/10.55522/jmpas.V15I4.7105.

ABSTRACT

Acitretin is a first-line retinoid for the management of psoriasis and other hyperkeratotic skin disorders; however, its therapeutic application is limited by poor aqueous solubility, inadequate skin retention, and dose-dependent systemic adverse effects following oral administration. The objective of the present study was to formulate and statistically optimize acitretin loaded nanostructured lipid carriers (NLCs) for improved topical drug delivery and prolonged local drug release. NLCs were synthesized via hot homogenization ultrasonication method and optimized by three factor-three level Box-Behnken experimental design to investigate effect of formulation variables on critical quality attributes like particle size and drug entrapment efficiency. The optimized formulation was well characterised for particle size distribution, polydispersity index, zeta potential, surface morphology, encapsulation efficiency, in vitro drug release and storage stability. The optimized NLCs showed nanosized particles with narrow size distribution, high drug encapsulation efficiency and suitable zeta potential, which suggested good colloidal stability. Scanning electron microscopy confirmed the formation of almost spherical nanoparticles with smooth surfaces and little agglomeration. In vitro release studies indicated a sustained release profile that was mainly controlled by diffusion-controlled kinetics, suggesting an efficient incorporation of the drug into the lipid matrix. Moreover, the optimized formulation showed good stability at the tested conditions and maintained its physicochemical properties during storage. The combined results indicate the potential of statistically optimized nanostructured lipid carriers as a topical delivery system for acitretin by increasing drug encapsulation, improving formulation stability and enabling controlled drug release, thus providing the possibility of improving the therapeutic efficacy while minimizing systemic exposure and related adverse effects in the treatment of chronic inflammatory skin disorders.

Keywords:

Acitretin, Nanostructured lipid carrier, Topical drug delivery, Box-Behnken design, Controlled release, Skin disorders.

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