Engineering of QbD driven and ultrasonically shaped lyotropic liquid crystalline nanoparticles for Apigenin in the management of skin cancer

Eur J Pharm Biopharm. 2022 Nov:180:269-280. doi: 10.1016/j.ejpb.2022.10.015. Epub 2022 Oct 20.

Abstract

Treatment of skin cancer demands targeted delivery without minimal systemic circulation for maximum therapeutic window. Dermal delivery with nano-formulation offers such advantages. Therefore, present study aims to formulate Lyotropic liquid crystalline nanoparticles (LLC NPs) loaded with Apigenin (API) for dermal delivery using quality by design (QbD) approach for effective permeation resulting in improved bioavailability. Apigenin loaded LLC NPs (API-LLC NPs) were formulated and optimized by applying risk assessment and design of experiments (Box-Behnken Design). The optimized API-LLC NPs showed particle size, PdI and entrapment efficiency of 287.7 ± 9.53 nm, 0.152 ± 0.051 and 80 ± 2.2 % respectively. The optimized API-LLC NPs were characterized for morphology and crystallinity using optical microscopy, TEM, DSC and PXRD. In vitro and ex vivo studies showed sustained release and better permeation profile. CLSM study presented better penetration of API-LLC NPs which were quantitatively confirmed with dermatokinetics. Cytotoxic efficacy assessed on B16F10 cell lines showed a dose-dependent efficacy of API-LLC NPs with an IC50 of 45.74 ± 0.05. In a nutshell, the developed API-LLC NPs exhibit excellent potential for targeting deeper skin layers thereby can be considered a promising topical drug delivery nanocarrier in the treatment and management of skin cancer.

Keywords: Apigenin; CLSM; Cytotoxicity; Dermal delivery; Liquid crystalline nanoparticles; Quality by design.

MeSH terms

  • Apigenin
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Drug Liberation
  • Humans
  • Nanoparticles* / chemistry
  • Particle Size
  • Skin Neoplasms* / drug therapy

Substances

  • Apigenin
  • Drug Carriers