Development of hydrocortisone succinic acid/and 5-fluorouracil/chitosan microcapsules for oral and topical drug deliveries

• Published in: Bioorganic & medicinal chemistry letters Vol. 22; no. 9; pp. 3213 - 3218
• Main Authors: Lam, Pik-Ling, Lee, Kenneth Ka-Ho, Wong, Raymond Siu-Ming, Cheng, Gregory Yin Ming, Cheng, Shuk Yan, Yuen, Marcus Chun-Wah, Lam, Kim-Hung, Gambari, Roberto, Kok, Stanton Hon-Lung, Chui, Chung-Hin
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 01-05-2012; Elsevier
• Subjects: 5-Fluorouracil; Administration, Oral; Administration, Topical; Animals; bioactive properties; Biological and medical sciences; Capsules - chemistry; chemical composition; Chitosan; corticotropin; cortisol; Drug delivery; Drug Delivery Systems - methods; drugs; fabrics; Fluorouracil; Fourier transform infrared spectroscopy; General pharmacology; Hydrocortisone; Hydrocortisone succinic acid; keratinocytes; Keratinocytes - cytology; Medical sciences; Mice; Microcapsule; Miscellaneous; oils; particle size; Pharmacology. Drug treatments; scanning electron microscopes; Skin - cytology; Skin - drug effects; Staphylococcus aureus; Succinic Acid; topical application; Hydrocortisone succinic acid; Drug delivery; Chitosan; 5-Fluorouracil; Microcapsule; Antineoplastic agent; Steroid; Drug carrier; Hydrocortisone; Local administration; Microparticle; Fluorouracil; Corticosteroid; Enzyme; Steroid hormone; Fluoropyrimidine derivatives; Transferases; Antiinflammatory agent; Oral administration; Enzyme inhibitor; Polymer; Thymidylate synthase; Biological activity; Antimetabolic; Methyltransferases; Adrenal hormone; Pyrimidine derivatives; Polysaccharide; Topical administration
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2012.03.031

We investigated that both oral and topical applications of chitosan-based microcapsules were tested using hydrocortisone succinic acid and 5-fluorouracil, respectively. Further uses of the drug loaded microcapsules may provide an efficiency deliverable tool for both oral and topical applications.
Recently, we demonstrated the safety use of calendula oil/chitosan microcapsules as a carrier for both oral and topical deliveries. We also reported the improved biological activity towards skin cells and Staphylococcus aureus of phyllanthin containing chitosan microcapsules. However, the possibility of both oral and topical applications was still necessary to be further studied. Here we investigated that both oral and topical applications of chitosan-based microcapsules were tested using hydrocortisone succinic acid (HSA) and 5-fluorouracil (5-FU), respectively. The drug loading efficiency, particle size, surface morphology and chemical compositions of both drug loaded microcapsules were confirmed by UV–vis spectrophotometer, particle size analyzer, scanning electron microscope and Fourier transform infrared spectroscopy. The in vitro release studies revealed that both HSA and 5-FU could be released form chitosan microcapsules. The mean adrenocorticotropic hormone concentration in HSA loaded microcapsule mice plasma was detected to be lower than that of water control. One hundred micrograms per milliliter of 5-FU containing microcapsules exhibited a stronger growth inhibition towards skin keratinocytes than that of free 5-FU. In vitro drug delivery model demonstrated the delivery of 5-FU from microcapsule treated textiles into nude mice skin. Further uses of the drug loaded microcapsules may provide an efficiency deliverable tool for both oral and topical applications.