Squalene-Containing Nanostructured Lipid Carriers Promote Percutaneous Absorption and Hair Follicle Targeting of Diphencyprone for Treating Alopecia Areata
- 855 Downloads
Diphencyprone (DPCP) is a therapeutic agent for treating alopecia areata. To improve skin absorption and follicular targeting nanostructured lipid carriers (NLCs) were developed.
Nanoparticles were characterized by size, zeta potential, molecular environment, differential scanning calorimetry (DSC), and nuclear magnetic resonance (NMR). In vitro and in vivo skin absorption experiments were performed. Fluorescence and confocal microscopes for imaging skin distribution were used.
NLCs with different designs were 208 ~ 265 nm with > 77% DPCP encapsulation. NLCs incorporating a cationic surfactant or more soybean phosphatidylcholine (SPC) showed higher lipophilicity compared to typical NLCs by Nile red emission. All NLCs tested revealed controlled DPCP release; burst release was observed for control. The formulation with more SPC provided 275 μg/g DPCP skin retention, which was greater than control and other NLCs. Intersubject deviation was reduced after DPCP loading into NLCs. Cyanoacrylate skin biopsy demonstrated greater follicular deposition for NLCs with more SPC compared to control. Cationic NLCs but not typical or SPC-containing carriers were largely internalized into keratinocytes. In vivo skin retention of NLCs with more SPC was higher than free control. Confocal imaging confirmed localization of NLCs in follicles and intercellular lipids of stratum corneum.
This work encourages further investigation of DPCP absorption using NLCs with a specific formulation design.
KEY WORDSalopecia areata diphencyprone hair follicles nanostructured lipid carriers percutaneous absorption
- 15.Wen CJ, Zhang LW, Al-Suwayeh SA, Yen TC, Fang JY. Theranostic liposomes loaded with quantum dots and apomorphine for brain targeting and bioimaging. Int J Nanomed. 2012;7:1599–611.Google Scholar
- 25.Lombardi Borgia S, Regehly M, Sivaramakrishnan R, Mehnert W, Korting HC, Danker K, et al. Lipid nanoparticles for skin penetration enhancement–correlation to drug localization within the particle matrix as determined by fluorescence and parelectric spectroscopy. J Contr Rel. 2005;110:151–63.CrossRefGoogle Scholar
- 34.Messenger AG. Alopecia areata. Eur J Dermatol. 2006;16:537–42.Google Scholar