Solubility Enhancement of Simvastatin through Surfactant Addition for Development of Hydrophobic Drug-Loaded Gelatin Hydrogel

This study aims to synthesize simvastatin hydrogel as drug delivery system with surfactant addition for improving solubility of simvastatin. Surfactants used in the study were the zwitterionic amino acid of arginine and nonionic surface-active agent of polysorbate 80. The solubility study was conducted by pouring of an excess mass of simvastatin into the solution of a surfactant in a conical flask. The sample was shaken up to 72 h in a mechanical water bath shaker at a varied temperature of 25, 40, and 50 °C. The amount of drug dissolved in solution was analyzed by UV/Visible spectrophotometer at 238 nm. The results showed that the simvastatin solubility is profoundly influenced by the surfactant type, surfactant concentration, and temperature. Polysorbate 80 exhibited as a better surfactant than arginine and an enhancement up to 1400 times, in respect of without any addition of a surfactant, was observed. Based on the solubility study, simvastatin-loaded gelatin hydrogel composite was formulated and the characterization (FTIR and SEM) showed the successful impregnation. The hydrogel microparticles of featured swelling indexes in the range of 2–6 for every patch and presented a sustained release profile.

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Development of Nifedipine Amorphous Solid Dispersion Composed of Surface-Active Agents

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.901.35 ◽

2021 ◽

Vol 901 ◽

pp. 35-39

Author(s):

Sukannika Tubtimsri ◽

Yotsanan Weerapol

Keyword(s):

Surface Active Agent ◽

Active Agent ◽

Amorphous Solid ◽

Drug Dissolution ◽

Amorphous Solid Dispersion ◽

Polysorbate 80 ◽

X Ray ◽

Surface Active Agents ◽

Surface Active ◽

Methacrylate Copolymer

The amorphous solid dispersions (ASDs) containing amino methacrylate copolymer and surface-active agents were prepared to improve the nifedipine (NDP) dissolution. The different types of surface-active agent i.e., polysorbates 80, sodium lauryl sulfate (SLS) and polyethylene glycol (PEG) 400 were used. In order to evaluate the ASDs formulation,powder X-ray diffractometry and thermal analysis to characterize NDP crystallinity in ASDs and the dissolution study of NDP have been performed to compare the dissolution profiles. The ASDs were kept for 6 months to investigate the stability. In the X-ray diffraction pattern, no peak was observed in all samples of ASDs. No peak was found in sample of all ASDs from the thermograms. These results suggest that the drug may be molecularly dispersed in matrix of amino methacrylate copolymer. The drug dissolution at 120 min, from ASDs without surface-active agent and NDP powder were 58.31% and 17.95%, respectively. The dissolved NDP from ASDs composed of SLS, polysorbate 80 and PEG400 were 96.25%, 88.86% and 75.32%, respectively. These results may occur due to the reduction of surface tension, the addition of the low amount of high efficiency of surface-active agent e.g., SLS (compared with PEG400 and polysorbate 80) provided the higher NDP dissolution. The content analysis of NDP in selected ASDs was studied at the end of 3 and 6 months, the NDP content remained unchanged after storage.

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