Purpose: To develop and evaluate the suitability of lecithin organogels containing aceclofenac for topical application and compare its In vitro and In vivo effects with conventionally used hydrogels.
Methods: The components and their concentration necessary for organogels formation were evaluated using phase diagram. Solubility of aceclofenac was determined. The In vitro skin permeation ability of aceclofenac from ethyl oleate based lecithin organogels [EO/lecithin organogel] and hydrogel was investigated. The In vivo characterization of ethyl oleate based organogel study was compared with that of hydrogel.The alterations in microstructure of organogels during diffusion study were elucidated. Viscosity and micellar size of the organogel sample were estimated. The safety of optimized organogel was determined using histopathological investigation.
Results: The flux calculated for skin permeation ability of aceclofenac was in the order EO/lecithin organogel > hydrogel. The In vivo results also demonstrated that organogels are more effective in faster drug release as compared to hydrogels. It was observed that viscosity of gels decreased with increasing stress .The size of micellar aggregation increased with water added and has been revealed in dynamic light scattering (DLS) study. The histopathological data showed that EO/lecithin organogel were safe enough for topical purpose.
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http://dx.doi.org/10.2174/156720109787048320 | DOI Listing |
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Guangdong Provincial Key Laboratory of New Drug Screening, NMPA Key Laboratory for Research and Evaluation of Drug Metabolism, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
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College of Life Science, South-Central Minzu University, No. 182, Minyuan Road, Hongshan District, Wuhan 430074, China.
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Radiopharmaceutical theranostics holds significant promise in tumor diagnosis and treatment, but suboptimal tumor uptake and retention remain a persistent limitation. We have conjugated a unique albumin binder to our previously developed heterodimeric precursor HX01 and achieved a novel precursor L6, aiming to prolong circulation time and enhance tumor accumulation and retention. However, we observed that the NGR sequence of L6 was gradually rearranged to iso-DGR under alkaline conditions, resulting in decreased stability.
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