The choice of excipients constitutes a major part of preformulation and formulation studies during the preparation of pharmaceutical dosage forms. The physical, mechanical, and chemical properties of excipients affect various formulation parameters, such as disintegration, dissolution, and shelf life, and significantly influence the final product. Therefore, several studies have been performed to evaluate the effect of drug-excipient interactions on the overall formulation. This article reviews the information available on the physical and chemical instabilities of excipients and their incompatibilities with the active pharmaceutical ingredient in solid oral dosage forms, during various drug-manufacturing processes. The impact of these interactions on the drug formulation process has been discussed in detail. Examples of various excipients used in solid oral dosage forms have been included to elaborate on different drug-excipient interactions.
Thermo-sensitive hydrogels are considered ideal for applications in the biomedical fields for their biocompatibility, flexibility, tissue-like water content, and reversible gelation property. By adjusting sufficient hydrophilic-hydrophobic balance in block copolymer structure, thermogel's critical gelation temperature can be modified to be near the physiological temperature, which makes it an appealing candidate for in situ gel depot. In this study, we report successful syntheses of novel multiple block copolymer compounds, denoted as dual-stimuli sensitive polymers (DSSPs), by copolymerizing Pluronic® P104 (7,100 Da) and 2,2-bis(aminoethoxy)propane (BAP) using diisocyanate linkers, L-lysine ethyl ester diisocyanate (DSSP-1) and 1,6-hexamethylene diisocyanate (DSSP-2). Through effective elongation of polymer chain lengths (DSSP-1: 41,760 Da, DSSP-2: 41,230 Da), Pluronic® P104's reversible thermal gelation properties were enhanced, as demonstrated by lowered critical gelation temperatures (DSSP-1: 36°C, DSSP-2: 38.7°C; 15 wt.%) that is near the physiological temperature. Furthermore, integration of acid-labile BAP allowed rapid pH-dependent degradation of the polymer, which was displayed by gel permeation chromatography (GPC) and release profiles of nile red and irinotecan from polymeric micelles and gels, respectively.
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