minoxidil-sulfate-ester and Alopecia

Polymeric nanofibers fabricated by electrospinning either blank (PVA) or loaded with minoxidil sulphate have yielded optimum fibers with an average diameter 273 nm, and 511 nm, respectively. Thermal analysis of nanofibers indicated no chemical interaction. The NMR spectrum confirmed stability of nanofiber as there were no interactions between functional groups. Prepared nanofibers showed a 47.4% encapsulation efficiency and 73% yield. In vitro drug release of minoxidil sulphate from nanofiber exhibited an initial burst release followed by a slower release pattern. Stability studies revealed that minoxidil nanofiber was stable if stored at room temperature and protected from light with only loss of 9.6% of its nominal concentration within 6 months. As a result, the prepared solid/colored formula serves as an ideal formulation for such instable drug in liquid formula taking the advantage of the attractiveness of beauty colored coverage, and the simple, and non-tousled application.

Topics: Alopecia; Drug Carriers; Drug Liberation; Humans; Minoxidil; Nanofibers; Polymers

Topical minoxidil is the only US FDA approved OTC drug for the treatment of androgenetic alopecia (AGA). Minoxidil is a pro-drug converted into its active form, minoxidil sulfate, by the sulfotransferase enzymes in the outer root sheath of hair follicles. Previously, we demonstrated that sulfotransferase activity in hair follicles predicts response to topical minoxidil in the treatment of AGA. In the human liver, sulfotransferase activity is significantly inhibited by salicylic acid. Low-dose OTC aspirin (75-81 mg), a derivative of salicylic acid, is used by millions of people daily for the prevention of coronary heart disease and cancer. It is not known whether oral aspirin inhibits sulfotransferase activity in hair follicles, potentially affecting minoxidil response in AGA patients. In the present study, we determined the follicular sulfotransferase enzymatic activity following 14 days of oral aspirin administration. In our cohort of 24 subjects, 50% were initially predicted to be responders to minoxidil. However, following 14 days of aspirin administration, only 27% of the subjects were predicted to respond to topical minoxidil. To the best of our knowledge, this is the first study to report the effect of low-dose daily aspirin use on the efficacy of topical minoxidil.

Topics: Administration, Cutaneous; Adult; Alopecia; Aspirin; Drug Interactions; Enzyme Inhibitors; Hair Follicle; Humans; Male; Minoxidil; Prodrugs; Risk Assessment; Sulfotransferases; Treatment Outcome; Young Adult

Although minoxidil (MX) is a drug known to stimulate hair growth, the treatment of androgenic alopecia could be improved by delivery strategies that would favor drug accumulation into the hair follicles. This work investigated in vitro the potential of iontophoresis to achieve this objective using MX sulfate (MXS), a more water-soluble derivative of MX. Passive delivery of MXS was first determined from an ethanol-water solution and from a thermosensitive gel. The latter formulation resulted in greater accumulation of MXS in the stratum corneum (skin's outermost layer) and hair follicles and an overall decrease in absorption through the skin. Anodal iontophoresis of MXS from the same gel formulation was then investigated at pH 3.5 and pH 5.5. Compared with passive delivery, iontophoresis increased the amount of drug reaching the follicular infundibula from 120 to 600 ng per follicle. In addition, drug recovery from follicular casts was threefold higher following iontophoresis at pH 5.5 compared with that at pH 3.5. Preliminary in vivo experiments in rats confirmed that iontophoretic delivery of MXS facilitated drug accumulation in hair follicles. Overall, therefore, iontophoresis successfully and significantly enhanced follicular delivery of MX suggesting a useful opportunity for the improved treatment of alopecia.

Topics: Administration, Cutaneous; Alopecia; Animals; Drug Delivery Systems; Hair Follicle; Iontophoresis; Male; Minoxidil; Rats; Rats, Wistar; Skin; Skin Absorption; Swine; Vasodilator Agents

Topics: Alopecia; Animals; Hair; Hair Color; Male; Mice; Mice, Inbred C3H; Minoxidil; Skin; Time Factors