Design of a Topically Applied Gel Spray Formulation with Ivermectin Using a Novel Low Molecular Weight Gelling Agent, Palmitoyl-Glycine-Histidine, to Treat Scabies

被引:14
作者
Dahlizar, Sabrina [1 ,2 ]
Futaki, Mika [3 ]
Okada, Akie [1 ]
Kadhum, Wesam Radhi [3 ]
Todo, Hiroaki [1 ,3 ]
Sugibayashi, Kenji [1 ,3 ]
机构
[1] Josai Univ, Grad Sch Pharmaceut Sci, 1-1 Keyakidai, Sakado, Saitama 3500295, Japan
[2] Syarif Hidayatullah State Islamic Univ Jakarta, Dept Pharm, Fac Med & Hlth Sci, Jalan Kertamukti 5, Ciputat 15419, Banten, Indonesia
[3] Josai Univ, Fac Pharm & Pharmaceut Sci, 1-1 Keyakidai, Sakado, Saitama 3500295, Japan
关键词
low-molecular weight gelling agent; ivermectin; gel spray formulation; skin concentration; thixotrophy; RESPONSIVENESS; PERMETHRIN; HYDROGELS; RELEASE;
D O I
10.1248/cpb.c17-00965
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Palmitoyl-glycine-histidine (Pal-GH) is a new low molecular weight gelling agent. It exhibits thixotropic behavior, low viscosity, and high dissolving properties for a wide range of hydrophilic to lipophilic drugs. Orally administered ivermectin (IVM) is used to treat scabies. However, this treatment is associated with well-known side effects, thus a study is awaited to search for alternative routes of administration. Although a topical formulation of IVM could be a candidate, it requires whole body application except the head and face for several hours on a daily basis. Therefore, in this study, we prepared a gel spray formulation containing IVM as an approach for application to large skin areas with a single spray application without further contact with the applied formulation. Pal-GH gel spray formulations were prepared from its aqueous solution by a heating and cooling method. Rheological behavior and physical appearance (spraying, spreading ability, volume of spraying, and homogeneity) of the prepared formulations were evaluated. Pal-GH gel with propylene glycol demonstrated impressive rheological properties (typical thixotropic behavior) with high hysteresis area among all the tested Pal-GH gels and spreading ability. The obtained IVM concentration in the skin after topical application of 0.1% IVM-containing Pal-GH formulation onto hairless rats was much higher than the reported therapeutic concentration obtained from oral administration in humans. These results suggested that topical application of IVM using a Pal-GH gel spray formulation could be an alternative to the conventional oral forms for the scabies treatment.
引用
收藏
页码:327 / 333
页数:7
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