NDLI: Preparation, Characterization, and In Vitro Permeation Study of Terbinafine HCl in Poloxamer 407-Based Thermogelling Formulation for Topical Application

Content Provider	Springer Nature Link
Author	Müller Goymann, Christel C.
Copyright Year	2011
Abstract	Upon topical administration, a high penetration rate of antifungal drug into the infected site is desirable to reduce treatment length and systemic side effects which occur especially after a prolonged peroral administration. Thermogelling formulations composed of poloxamer 407, medium chain triglycerides, isopropyl alcohol, dimethyl isosorbide, and water for topical application were developed, and a lipophilic drug terbinafine HCl (TBF) was incorporated. Previously, a remarkable high permeation rate of a hydrophilic drug 5-aminolevulinic acid from this vehicle was evident compared to different creams from German Pharmacopoeia. By varying the composition of vehicle constituents, a broad range of consistencies and appearances was obtained. Up to 4% TBF could be solubilized in the vehicle. TBF fluxes at steady state across human stratum corneum from these formulations were higher than those from the German Pharmacopoeia Basiscreme Deutscher Arzneimittel Codex and a marketed product at similar concentration of 1%. TBF fluxes increased along with a higher content of TBF in the formulation. The amount of TBF retained in stratum corneum was higher compared to those from both standards of comparison (p < 0.01). The thermodynamic activity of TBF in the thermogelling formulation was lower compared to those in other formulations. Therefore, the nature of the vehicle and its interaction with TBF are suggested to play a significant role in explaining higher fluxes along with higher TBF content. Differential scanning calorimetry measurements revealed comparable T2 and T3 endothermic shifts from all examined formulations suggesting equal influences to the skin lipids.
Starting Page	496
Ending Page	506
Page Count	11
File Format	PDF
Journal	AAPS PharmSciTech
Volume Number	12
Issue Number	2
e-ISSN	15309932
Language	English
Publisher	Springer US
Publisher Date	2011-04-09
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	permeation poloxamer 407 stratum corneum terbinafine HCl thermogelling formulation Pharmacy Biochemistry Biotechnology Pharmacology/Toxicology
Content Type	Text
Resource Type	Article

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