Oleic Acid Nanovesicles of Minoxidil for Enhanced Follicular Delivery

Abstract

Current topical minoxidil (MXD) formulations involve an unpleasant organic solvent which causes patient incompliance in addition to side effects in some cases. Therefore, the objective of this work was to develop an MXD formulation providing enhanced follicular delivery and reduced side effects. Oleic acid, being a safer material, was utilized to prepare the nanovesicles, which were characterized for size, entrapment efficiency, polydispersity index (PDI), zeta potential, and morphology. The nanovesicles were incorporated into the emugel Sepineo® P 600 (2% w/v) to provide better longer contact time with the scalp and improve physical stability. The formulation was evaluated for in vitro drug release, ex vivo drug permeation, and drug deposition studies. Follicular deposition of the vesicles was also evaluated using a differential tape stripping technique and elucidated using confocal microscopy. The optimum oleic acid vesicles measured particle size was 317 ± 4 nm, with high entrapment efficiency (69.08 ± 3.07%), narrow PDI (0.203 ± 0.01), and a negative zeta potential of −13.97 ± 0.451. The in vitro drug release showed the sustained release of MXD from vesicular gel. The skin permeation and deposition studies revealed superiority of the prepared MXD vesicular gel (0.2%) in terms of MXD deposition in the stratum corneum (SC) and remaining skin over MXD lotion (2%), with enhancement ratios of 3.0 and 4.0, respectively. The follicular deposition of MXD was 10-fold higher for vesicular gel than the control. Confocal microscopy also confirmed the higher absorption of rhodamine via vesicular gel into hair follicles as compared to the control. Overall, the current findings demonstrate the potential of oleic acid vesicles for effective targeted skin and follicular delivery of MXD.

Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels

“…In the last decade, many experimental studies have focused on the improvement of topical administration of MXD by different strategies: nanoemulsions [ 40 , 41 ], nanovesicles [ 42 ], nanostructured lipid carriers [ 43 ], electrodynamic microneedles [ 44 ], the synergistic effect of other drugs, e.g., tretinoin [ 45 ] and others [ 46 ]. The study of Maitra et al [ 21 ] brought positive results in terms of MXD enhancement in permeation through the skin (in vitro, ex vivo, in vivo) from ME-based formulation consisting of oleic acid, PEG 600, Span 20 and water.…”

Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia

“…An accurate volume (1 mL) of SV-loaded nanospanlastic dispersions containing entrapped SV or the equivalent concentration of SV aqueous dispersion were placed in the donor partition over the semi-permeable membrane. The receptor partition contained 100 mL of phosphate buffer solution (pH = 7.4) as a receptor medium [ 26 , 27 ] which rotated at 100 rpm at 32 ± 0.5 °C during the study to mimic the temperature of the scalp skin [ 28 , 29 ]. A total of 1 mL of aliquot was withdrawn at different time points and replaced by the same volume of phosphate buffer to maintain sink conditions and constant volume of the receptor medium.…”

Hybrid Oleic Acid‐Graphene Quantum Dot Vesicles for Drug Delivery

“…In many cases, oleic acid is combined with other materials like cholesterol or phospholipid to form such systems. But the hybrid vesicle system (OA‐GQD)shown here consisting of oleic acid and graphene quantum dots gives 98.3% entrapment efficiency which is quite high compared to previously reported systems ,,,…”