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Preservation of Anticancer and Immunosuppressive Properties of Rapamycin Achieved Through Controlled Releasing Particles.
Fan, Yan Liang; Hou, Han Wei; Tay, Hui Min; Guo, Wei Mei; Berggren, Per-Olof; Loo, Say Chye Joachim.
Afiliación
  • Fan YL; Nanyang Institute of Technology in Health & Medicine, Interdisciplinary Graduate School, Nanyang Technological University, Singapore, Singapore.
  • Hou HW; School of Materials Science and Engineering, Nanyang Technological University, 50 Nanyang Avenue, Singapore, 639798, Singapore.
  • Tay HM; Lee Kong Chian School of Medicine, Nanyang Technological University, Singapore, Singapore.
  • Guo WM; Lee Kong Chian School of Medicine, Nanyang Technological University, Singapore, Singapore.
  • Berggren PO; The Agency for Science, Technology and Research, Biotransformation Innovation Platform, Singapore, Singapore.
  • Loo SCJ; Lee Kong Chian School of Medicine, Nanyang Technological University, Singapore, Singapore.
AAPS PharmSciTech ; 18(7): 2648-2657, 2017 Oct.
Article en En | MEDLINE | ID: mdl-28251512
ABSTRACT
Rapamycin is commonly used in chemotherapy and posttransplantation rejection suppression, where sustained release is preferred. Conventionally, rapamycin has to be administered in excess due to its poor solubility, and this often leads to cytotoxicity and undesirable side effects. In addition, rapamycin has been shown to be hydrolytically unstable, losing its bioactivity within a few hours. The use of drug delivery systems is hypothesized to preserve the bioactivity of rapamycin, while providing controlled release of this otherwise potent drug. This paper reports on the use of microparticles (MP) as a means to tune and sustain the delivery of bioactive rapamycin for up to 30 days. Rapamycin was encapsulated (100% efficiency) in poly(lactic-co-glycolic acid) (PLGA), polycaprolactone (PCL), or a mixture of both via an emulsion method. The use of different polymer types and mixture was shown to achieve a variety of release kinetics and profile. Released rapamycin was subsequently evaluated against breast cancer cell (MCF-7) and human lymphocyte cell (Jurkat). Inhibition of cell proliferation was in good agreement with in vitro release profiles, which confirmed the intact bioactivity of rapamycin. For Jurkat cells, the suppression of cell growth was proven to be effective up to 20 days, a duration significantly longer than free rapamycin. Taken together, these results demonstrate the ability to tune, sustain, and preserve the bioactivity of rapamycin using MP formulations. The sustained delivery of rapamycin could lead to better therapeutic effects than bolus dosage, at the same time improving patient compliance due to its long-acting duration.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Sistemas de Liberación de Medicamentos / Sirolimus / Inmunosupresores / Antineoplásicos Límite: Humans Idioma: En Revista: AAPS PharmSciTech Asunto de la revista: FARMACOLOGIA Año: 2017 Tipo del documento: Article País de afiliación: Singapur

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Sistemas de Liberación de Medicamentos / Sirolimus / Inmunosupresores / Antineoplásicos Límite: Humans Idioma: En Revista: AAPS PharmSciTech Asunto de la revista: FARMACOLOGIA Año: 2017 Tipo del documento: Article País de afiliación: Singapur