Encapsulation of erythromycin and bacitracin antibiotics into natural sporopollenin microcapsules: antibacterial, cytotoxicity, and release studies for enhanced bioavailability.

Nature produces large quantities of superbly complex and highly reliable microcapsules. The micrometre-sized spores are one example of these robust capsules. The encapsulation of erythromycin (EM) and bacitracin (BAC) antibiotics into the sporopollenin (LCS) extracted from these spore species is explored for the first time. The LCS microparticles are extensively characterised before and after loading using SEM, CLSM, TGA and FTIR techniques. The loading capacity and entrapping efficiency of EM were 16.2 and 32.4%, respectively. The antibacterial activities of pure antibiotics, empty LCS and the antibiotic-loaded LCS were evaluated against (Gram-positive), (Gram-negative), and (Gram-negative) human pathogenic bacterial strains. A remarkable increase in the antibacterial fold activity of both EM- and BAC-loaded LCS compared to that of the pure antibiotics is observed. Crucial for drug delivery applications, empty LCS, EM- and BAC-loaded LCS were found to be nontoxic against human epithelial colorectal adenocarcinoma cells Caco-2 as revealed by the cytotoxicity evaluation. The release mechanism of EM in pH 7.4 showed a deviation from Fick's law. release of EM from EM-loaded LCS (an oral dose of 50 mg kg) revealed high values of the area under the plasma concentration-time curve (AUC and AUC were 1620 and 2147 μg h L, respectively) indicative of the enhanced EM bioavailability. The successful loading of antibiotics into the nontoxic LCS and the enhanced bioavailability can open up intriguing applications in oral and topical drug delivery strategies.