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Hair follicle (HF), one of the skin appendages, has received a lot of attention to be a new target and pathway for drug delivery. The development of hair follicle targeted drug delivery system (HFTDDS) through percutaneous permeation is particularly important for skin diseases derived from HF such as acne, hair loss, and folliculitis for their on-site action. This review describes the structure and physiological function of HF, the microenvironment of HF, and factors affecting HF permeation. Multiple nanoformulations used to improve the HF permeation and technologies to characterize the HF permeation were introduced. The latest advance of HFTDDS based on nanoformulations were systematically summarized and analyzed in the treatment of acne and hair loss. Finally, the challenges of formulating HFTDDS were discussed. The review is expected to provide some ideas and references for developing delivery systems for treating skin diseases derived from HF.
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Objective:To investigate the percutaneous permeability of sinomenine hydrochloride （SNH） and optimize the parameters of electroporation to achieve the best permeation enhancing effect on SNH. Method:The percutaneous permeability of SNH and the enhancement effect of electroporation were studied by <italic>in vitro</italic> diffusion cell method， and the enhancement effect of electroporation was further evaluated by <italic>in vivo</italic> study in mice. Result:Under steady-state condition， the permeation rates of SNH in stripped skin and intact skin of hairless mice were （385.81±12.88）， （0.88±0.20） μg·cm<sup>-2</sup>·h<sup>-1</sup>， respectively. The permeation rate in stripped skin was 438 times higher than that in intact skin. The results of percutaneous permeation kinetics analysis showed that the solubility and diffusion coefficient of SNH in stratum corneum were relatively low， which were （70.82±9.63）×10<sup>3</sup> g·m<sup>-3</sup> and （3.07±1.52）×10<sup>-14</sup> cm<sup>2</sup>·s<sup>-1</sup>， respectively. Under the optimized electroporation conditions （voltage of 72 V， time of 60 min）， the 24 h cumulative permeation amount of SNH through skin of mice was （10 008.39±1 961.57） μg·cm<sup>-2</sup>， and the steady-state permeation rate was （456.01±51.26） μg·cm<sup>-2</sup>·h<sup>-1</sup>， which were 5.4 times and 5.1 times higher than those of blank group， respectively. <italic>In vivo</italic> studies in mice showed that the contents of SNH in skin and muscle of electroporation group were 2.0 times and 1.5 times higher than those of blank group. Conclusion:The low solubility and low diffusion coefficient of SNH in the stratum corneum are the main factors hindering the percutaneous permeation of SNH. Electroporation can significantly increase the percutaneous permeation of SNH and its retention in skin and muscle of mice.
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Objective: To prepare celecoxib hotmelt pressure sensitive adhesive (HMPSA), and investigate the quality. Methods:Celecoxib HMPSA was prepared using styrene-isoprene-styrene triblock copolymer (SIS) as the chief material, and the quality of HMP-SA was inspected with stickiness, peel strength, melt temperature and percutaneous permeation rate in vitro as the indices. Results:The stickiness of celecoxib HMPSA was (17.79 ±0.25)N, the peel strength was (2.81 ±0.49) N·cm-2, the melt temperature was 90. 8 ± 1. 9℃, and the percutaneous permeation rate in 24h was (18. 77 ± 1. 51) mg·cm-2. Conclusion: The HMPSA is suitable for the preparation of TDDS of celecoxib.
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Objective: To explore the optimum preparation process of triptolide nanometer coating agent. Methods: Optimum preparation process was investigated by uniform design with the amount of film forming material such as polyethylene glycol 124 (PVA124), carbomer, CMC-Na, and the mixing time as investigating factors, and with uniformity, film-forming ability, and peeling strength as indexes. We conducted sc simulation experiment in vitro to investigate the percutaneous penetration process of triptolide nanometer coating agent. Results: The best way to prepare triptolide nanometer coating agent is that we use glycerol monostearate 1.6 g, glycerin 0.25 g, PVA124 3.9 g, Carbomer 0.6 g, CMC-Na 0.9 g, and mix them in 150 min. With above preparation process, we can achieve better coating agent. JS was 0.350 µg/(cm2·h) and the cumulative permeation quantity in 24 h was 11.534 µg/cm2. Conclusion: Using the optimum preparation process, we can get better triptolide nanometer coating agent, which is uniform, easy coating,good adhesion with skin, strong flexibility, and drying soon.
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Objective: To clarify the percutaneous absorption characteristics of sinomenine hydrochloride (SIN-HCl) PEGylated transfersomes (SHPT) edge activated by volatile oils and to compare with others carriers. Methods: Various formulations of transfersomes [The representative formulations of SHPT contained different quantity of volatile oils including SHPT-A, SHPT-B, and SHPT-C; non-PEGylated transfersomes (SHT-A and SHT-B) corresponded to SHPT-A and SHPT-B; SHDT was edge activated by sodium deoxycholate], PEGylated liposomes (SHPL), and liposomes (SHLS) were prepared by ethanol injection method. Characterization of vesicles was based on results from particle size, morphology, elasticity, and entrapment efficiency (EE) studies. Elasticity was measured by constant pressure extrusion method and EE was measured by HPLC combined with centrifugation ultrafiltration. The skin permeation test was carried out with a Franz diffusion cell fitted with excised rat skin. The effects of vesicle types (SHPT, SHDT, SHLS, and SIN-HCl aqueous solution), DSPE-PEG 2000, and volatile oil in the SHPT on percutaneous permeation of SIN-HCl were investigated. Results: The SIN-HCl transfersomes and liposomes were mainly unilamellar vesicles with roundish shape and average size of 93-118 nm, without gathering property. The entrapment efficiency was of 11%-40%. The elasticity order of vesicles was SHPT-B > SHDT ≈ SHPT-A > SHT-B > SHT-A ≈ SHPL > SHLS > SHPT-C. The steady-state drug percutaneous permeation rate [J (μg∙cm-2∙h-1)] order of different vesicles was SHT-B (19.10 ± 5.74) > SHPT-B (17.06 ± 0.34) > SHDT (15.16 ± 0.55) > SHT-A (10.96 ± 0.99) > SHPT-A (9.42 ± 1.09) > SHLS (3.90 ± 0.67) > SHPT-C (3.51 ± 0.37) > SIN-HCl aqueous solution (2.26 ± 0.94). The cumulative permeated percentages [Qe (36 h)] of SHT-B and SHPT-B were (89.79 ± 6.67)%, and (84.01 ± 6.77)%, respectively. The Qe (36 h) of SHDT, SHLS, SHPT-C and SIN-HCl aqueous solution were (73.98 ± 10.55)%, (20.29 ± 3.21)%, (15.45 ± 3.04)%, and (10.33 ± 2.91)%, respectively. The lag time of SHPT-A, SHPT-B, SHT-A, SHT-B, and SHDT (0.3-0.6 h) were significantly reduced, compared to SHLS and SIN-HCl aqueous solution (3.5-3.8 h). Conclusion: SHPT edge activated by appropriate volatile oils has good elasticity and percutaneous absorption characteristics, which is better than that of liposomes and transfersomes edge activated by sodium deoxycholate to different degrees.
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Objective: To establish the key conditions for the determination of percutaneous absorption of Panax notoginseng saponins (PNS) in transfersomes (TFS) by in vitro skin permeation method and clarify its percutaneous absorption characteristics. Methods: The film hydration-dispersion method was used to prepare PNS TFS and liposomes (LPS). Their physico-chemical properties were characterized. The drug content and sample volume of PNS TFS for in vitro skin permeation experiments were screened. The effects of vesicle type (TFS or LPS), size of the TFS, and formulation amount of sodium deoxycholate (DOC) on percutaneous permeation of PNS were investigated. Results: The TFS and LPS were mainly unilamellar vesicles with roundish shape and size of (121.2 ± 4.5) and (113.9 ± 2.9) nm, without gathering property. According to the cumulative permeated quantity (Qn) and steady-state percutaneous permeation rate (J) of the assayed ingredients, the appropriate PNS content in the TFS was 500 mg and sample volume was 0.5 mL. Compared with those of the LPS, the Qn values of each assayed component (ginseng saponin Rg1, ginseng saponin Rb1, ginseng saponin Re, PNS R1) in PNS of the TFS were high, and the J values of the assayed components in TFS were about 2-3 times of those in the LPS. The Qn and J values of the assayed components in the TFS with an average size of 120 nm were obviously higher than those of the assayed components in the TFS with an average size of 250 nm. The Qn and J values of the assayed components in PNS TFS with large amount of DOC were prominently higher than those containing small amount of DOC, and the increase ratios of different assayed components were different. Conclusion: In vitro skin permeation method is suitable for the determination of percutaneous absorption of PNS in TFS. The TFS promote drug percutaneous permeation stronger than the LPS and the promotion increases with an appropriate increase of the amount of DOC and decrease of vesicle size of the TFS.
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oleic acid, and 2% Azone plus 10% oleic acid had the strongest effect in all. Conclusion 2% Azone plus 10% oleic acid as the enhancer of SG is the best.