1. DoE-based development, physicochemical characterization, and pharmacological evaluation of a topical hydrogel containing betamethasone dipropionate microemulsion.
- Author
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Tung NT, Vu VD, and Nguyen PL
- Subjects
- Administration, Topical, Animals, Anti-Inflammatory Agents, Non-Steroidal administration & dosage, Anti-Inflammatory Agents, Non-Steroidal chemistry, Betamethasone administration & dosage, Betamethasone chemistry, Betamethasone pharmacology, Cellulose administration & dosage, Cellulose chemistry, Chemistry, Physical, Drug Carriers administration & dosage, Drug Carriers chemistry, Drug Carriers pharmacology, Emulsions administration & dosage, Emulsions chemistry, Emulsions pharmacology, Hydrogels administration & dosage, Hydrogels chemistry, Male, Mice, Particle Size, Rabbits, Rats, Rheology, Skin drug effects, Solubility, Surface Properties, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Betamethasone analogs & derivatives, Cellulose pharmacology, Edema drug therapy, Hydrogels pharmacology
- Abstract
This study was performed to achieve two primary goals: First, a microemulsion containing betamethasone dipropionate was optimized using the quality by design approach. Second, a hydrogel-containing microemulsion was developed using cellulose derivatives, and its anti-inflammatory and skin irritation effects were evaluated. Face-centered central composite design was used to investigate the impacts of two independent variables (oleic acid and ratio of surfactant to cosolvent, S/CoS) on three dependent variables (skin deposition, flux of BMD, and microemulsion droplet size). The microemulsion including oleic acid at a low level (coded with -1) and S/CoS at a high level (coded with +1) was considered optimal since it was the most effective in terms of skin deposition and flux of BMD. Different cellulose derivatives (HPMC E6, HEC, NaCMC, and CMC) were screened to prepare a hydrogel-containing microemulsion based on four properties: flux and skin deposition of BMD, hydration of stratum corneum, and rheological properties of hydrogel-containing microemulsion (ME-hydrogel). The anti-inflammatory effect and flux of BMD from optimal ME-hydrogel with carboxymethyl cellulose as the hydrogel-forming agent were then compared to those of the hydrogel-containing solid lipid nanoparticles (SLN-hydrogel) and nanostructure lipid carriers (NLC-hydrogel). The percentage of edema inhibition declined proportionally with flux of BMD in the following order: ME-hydrogel (44.56 ± 8.08%) > NLC-hydrogel (35.93 ± 7.22%) > SLN-hydrogel (25.68 ± 9.05%)., (Copyright © 2019 Elsevier B.V. All rights reserved.)
- Published
- 2019
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