Abstract
Lipidic implants are valuable controlled delivery systems that present good biocompatibility and are useful for long-lasting therapies. However, these promising systems can present inflexible drug release profiles that limit their performance. Thus, finding new materials to overcome this drawback is crucial. Herein, lipidic implants containing caffeine and poorly soluble salicylic acid and rutin were developed. The inclusion of Gelucire® 50/02, sucrose, and two biobased ionic liquids, [Cho][Phe] and [Cho][Glu], were evaluated as a mean to improve the performance of the systems. The formulation procedure, dye content distribution, drug content, drug release, water content, and lipidic erosion of the developed systems were assessed. AFM analysis of the implants containing ILs was also performed. The results demonstrated that neither Gelucire® 50/02 nor sucrose were suitable tools to improve the drug release profile. In contrast, the ILs proved to be promising materials for multiple reasons; not only did they facilitate the formulation and incorporation of the studied drugs into the implants, but they also allowed a more suitable release profile, with [Cho][Glu] allowing a higher drug release due to its ability to increase surface wrinkling. Hence, this study showcases ILs as multitalented materials in lipid-based drug implants.
Highlights
Accepted: 26 July 2021The pharmaceutical industry has always sought to develop drug delivery systems that allow for a prolonged and effective therapeutic effect to ensure less adverse effects and less frequency of administration
The lipidic implants are produced with lipids that contribute to a higher biocompatibility and low toxicity compared to polymeric implants [3,4,5,6]
Several lipidic implants with different compositions, namely different release adjuvants (Gelucire® 50/02 or sucrose), and in the presence or absence of two biobased ionic liquids (ILs) derived from natural amino acids ([Cho][Phe] or [Cho][Glu]) were prepared
Summary
Accepted: 26 July 2021The pharmaceutical industry has always sought to develop drug delivery systems that allow for a prolonged and effective therapeutic effect to ensure less adverse effects and less frequency of administration. There are various studies focused on lipidic implants due to their attractive properties compared to polymeric ones [3,4,5,6] Apart from their low toxicity and good biocompatibility, due to the presence of lipids that are constituents of the organism, their ability for drug protection and flexibility in choosing different excipients in the formulation process represent advantages [3,4,5,6,7,8].
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