Enhanced skin penetration of Finasteride loaded DMSO-liposomes for the treatment of androgenic alopecia: comparison with conventional liposomes.

Long-term treatment with finasteride (FIN) for androgenic alopecia is restricted due to its systemic side effects. To address this problem, DMSO-modified liposomes were prepared in the present study to improve the topical delivery of FIN. DMSO-liposomes were prepared by a modification of the ethanol injection method. It was hypothesized that the permeation-enhancing property of DMSO could promote drug delivery to deeper skin layer where hair follicles are present. Liposomes were optimized by quality by design (QbD) approach and biologically evaluated in a rat model of testosterone-induced alopecia. Optimized DMSO-liposomes were spherical and had mean vesicle size, zeta potential, and entrapment efficiency of 330.1 ± 1.5, -14.52 ± 1.32, and 59.02 ± 1.12%, respectively. Biological evaluation on testosterone-induced alopecia and skin histology shows that follicular density and anagen/telogen (A/T) ratio were increased in rats treated with DMSO-liposomes as compared to FIN-liposomes without DMSO and an alcoholic solution of FIN applied topically. DMSO-liposomes could be promising skin delivery vehicles for FIN or similar drugs.

Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables.

Finasteride (FIN), a 5-α reductase enzyme inhibitor is mainly used orally for the treatment of androgenic alopecia and benign prostate hyperplasia. The present study was undertaken for systematic optimization and assessment of the designed nanostructured lipid carriers (NLC) to enhance follicular delivery of FIN by topical administration. The NLCs were prepared by microemulsion method, by employing a 33 Box-Behnken design and subsequently confirmed by ANOVA analysis. Compritol ATO-888 and Fenugreek oil were selected as the solid lipid and liquid lipid respectively for the fabrication of NLCs. The formulations were characterized for particle size, zeta potential, entrapment efficiency, storage stability and in vitro drug release profile. Morphological profile of the NLCs nanocarriers was studied by transmission electron microscopy (TEM). The Fourier Transform Infrared Spectroscopy (FT-IR) spectrum and differential scanning calorimetry (DSC) thermogram demonstrated that FIN entrapment within NLCs was devoid of chemical interaction with the components. The prepared NLCs had satisfactory particle dimensions, zeta potential and entrapment efficiency. The numerical optimization process indicated the optimal NLC composition with 3 mg of SPC, 6 mg lipid and 5 mg of drug. NLCs loaded with FIN had acceptable particle size at 379.8 nm, zeta potential of -37.1 mV and an entrapment efficiency of 84%. Transmission electron microscopy indicated the spherical morphology. In vitro release profile indicated a fast initial release and subsequently a prolonged release of FIN from the carrier for 24 h. The release kinetics data displayed a Higuchi diffusion release model with the best match R2 value (0.848). Short-term stability tests conducted over 4 weeks at 6° and 25 °C demonstrated that the formulation could retain their initial properties during the test period.

Nano-Lipidic Carriers as a Tool for Drug Targeting to the Pilosebaceous Units.

The pilosebaceous unit is the triad comprising of hair follicle, arrector pilli muscle, and sebaceous gland. Drug delivery to and through the hair follicles has garnered much attention of the researchers and the hair follicles represent an attractive target site via topical applications. They are bordered by capillaries and antigenpresenting cells, connected to the sebaceous glands and the bulge region of the hair follicle anchors the stem cells. The nano lipid carriers have the propensity to penetrate through the skin via transcellular route, intracellular route and follicular route. It has been established that nano lipid carriers have the potential for follicular drug delivery and provide some advantages over conventional pathways, including improved bioavailability, enhanced penetration depth, fast transport into the skin, tissue targeting and form a drug reservoir for prolonged release. This review describes the pilosebaceous unit (PSU) and related diseases and the recent lipid-based nanotechnology approaches for drug delivery to the follicular unit as well as related issues. Different types of nano lipid carriers, including ethosomes, liposomes, nanoparticles, solid lipid nanoparticles (SLNs), and nano lipid carriers (NLCs) have been reported for follicular drug delivery. Targeted drug delivery with nano-lipid carriers has the potential to augment the efficacy of drugs/bioactives to treat diseases of PSU. This review systematically introduces the activities of different formulations and the use of nano lipid carriers in treating PSU related disorders like alopecia, acne, and hirsutism.