Follicular delivery of spironolactone via nanostructured lipid carriers for management of alopecia

Abstract

Spironolactone (SL) is a US Food and Drug Administration-approved drug for the treatment of hypertension and various edematous conditions. SL has gained a lot of attention for treating androgenic alopecia due to its potent antiandrogenic properties. Recently, there has been growing interest for follicular targeting of drug molecules for treatment of hair and scalp disorders using nanocolloidal lipid-based delivery systems to minimize unnecessary systemic side effects associated with oral drug administration. Accordingly, the objective of this study is to improve SL efficiency and safety in treating alopecia through the preparation of colloidal nanostructured lipid carriers (NLCs) for follicular drug delivery. SL-loaded NLCs were prepared by an emulsion solvent diffusion and evaporation method using 2 3 full factorial design. All of the prepared formulations were spherical in shape with nanometric size range (215.6–834.3 nm) and entrapment efficiency >74%. Differential scanning calorimetry thermograms and X-ray diffractograms revealed that SL exists in amorphous form within the NLC matrices. The drug release behavior from the NLCs displayed an initial burst release phase followed by sustained release of SL. Confocal laser scanning microscopy confirmed the potential of delivering the fluorolabeled NLCs within the follicles, suggesting the possibility of using SL-loaded NLCs for localized delivery of SL into the scalp hair follicles.

Trans-nasal zolmitriptan novasomes: in-vitro preparation, optimization and in-vivo evaluation of brain targeting efficiency

“…One drop of dispersion was deposited on the surface of a carbon-coated copper grid and left to adhere on the carbon substrate for 1 min and any excess of dispersion was removed by a tip of filter paper (Tavano et al, 2013;Shamma & Aburahma, 2014).…”

“…ZT, Span Õ 80, stearic acid, cholesterol and lyophilized ZT loaded novasomes were subjected to DSC (PerkinElmer, Waltham, MA). Approximately 4 mg of samples were analyzed in sealed aluminum pans in the temperature range from 30 to 300 C at a heating rate of 10 C/min under inert nitrogen flow (25 mL/min) (Shamma & Aburahma, 2014).…”

Spironolactone loaded nanostructured lipid carrier gel for effective treatment of mild and moderate acne vulgaris: A randomized, double-blind, prospective trial

“…Clinical studies with alcoholic topical formulation of SP have been previously reported and the results demonstrate beneficial effects in patients with acne without any systemic hormonal changes [3,12,13]. Shamma and Aburahma used spironolactone loaded NLC for follicular targeting of drug molecules for the management of alopecia and they successfully showed the presence of SP in the scalp hair follicles and decreasing androgen production within sebaceous glands and blocking the androgen receptor in dermal papillae [14]. The efficacy of SP gel 5% in the treatment of facial acne also showed that total lesion count and acne severity index reduced significantly however, efficacy on non-inflammatory lesion (comedones) was more effective than on inflammatory ones (papules and pustules) because of poor ability of SP penetration to specific micro environmental conditions in the inflammatory acne lesions [13].…”

Current application of phytocompound-based nanocosmeceuticals for beauty and skin therapy

“…Recently, a nanocosmeceutical-based approach of promoting hair growth was achieved using delivery technologies, such as niosomes and liposomes, to hair follicular cells. [106][107][108][109][110][111][112][113] Curcumin-based liposomes were constructed and had 70% enhanced penetration of the curcumin to the hair growth, irrespective of liposomes type in the size range of 213-320 nm. 114 Similarly, a curcumin-based cyclodextrin complex also showed enhanced follicle penetration and hair growth enhancement.…”