SKIN TARGETING OF AN OPTIMIZED CAFFEINE NANOSTRUCTURED LIPID CARRIER WITH IMPROVED EFFICIENCY AGAINST CHEMOTHERAPY INDUCED ALOPECIA

AMNA MOHAMED MAKKY; EMAN SADDAR EL-LEITHY; DOAA GALAA HUSSEIN; ABEER KHATTAB

doi:10.22159/ijap.2022v14i4.44681

Authors

AMNA MOHAMED MAKKY Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
EMAN SADDAR EL-LEITHY Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Cairo, Egypt, Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Ain-Helwan, Cairo 11795, Egypt
DOAA GALAA HUSSEIN Department of Pharmaceutics, Egyptian Drug Authority, Cairo, Egypt
ABEER KHATTAB Department of Pharmaceutics, Egyptian Drug Authority, Cairo, Egypt

DOI:

https://doi.org/10.22159/ijap.2022v14i4.44681

Keywords:

Caffeine, Topical, Alopecia, Nanostructured lipid carriers (NLCs)

Abstract

Objective: The current investigation was designed to develop and optimize caffeine-loaded nanostructured lipid carriers (NLCs) for topical alopecia treatment.

Methods: Screening of drug solubility in various excipients was executed. The 2³ full factorial design was employed for NLCs optimization. Lipid type, surfactant type, and drug concentration were the independent variables. Entrapment efficiency (EE), particle size, polydispersity index (PDI) and % drug release were the chosen responses. Physiochemical evaluation, in vitro release, ex-vivo permeation, and stability study were achieved.

Results: The solubility of caffeine in stearic acid and glyceryl monostearate (GMS) was 47.11±3.048 and 32.67±2.955 mg/g, respectively. Oleic acid: garlic oil mixture at a ratio of 1:1 v/v was the oily phase. Tween 80 and Cremophor EL, Transcutol HP, carbonate buffer (pH 10.8 and ionic strength 200 mmol) were chosen as a surfactant, co-surfactant, and aqueous phase, respectively. The optimized formula showed particle size, %EE, PDI, zeta potential of 358 nm±1.45, 72.55 %±0.12, 0.912±0.030,-24.8 mv±0.70, respectively. The % release was 92.9±4.9 % after 2 h. Confocal laser scanning microscopy showed an improved permeation of caffeine-loaded NLCs to the whole skin layers.

Conclusion: The histological examination proved the efficiency of caffeine NLCs optimized formula in promoting hair growth compared to the market formula.