Poly(ethylene glycol) enclatherated pectin-mucin submicron matrices for intravaginal anti-HIV-1 drug delivery

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• 作者：Felix Mashingaidze^a ; Yahya E. Choonara^a ; Pradeep Kumar^a ; Lisa C. du Toit^a ; Vinesh Maharaj^b ; Eckhart Buchmann^c ; Viness Pillay^a ; ^{viness.pillay@wits.ac.za" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Anti-HIV-1 ; Zidovudine ; Pectin ; Mucin ; Poly(ethylene glycol) ; Intravaginal delivery ; Submicron matrices
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：30 April 2016
• 年：2016
• 卷：503
• 期：1-2
• 页码：16-28
• 全文大小：3099 K

文摘

This paper explores the potential of polyethylene glycol enclatherated pectin-mucin (PEG-encl-PEC:MUC) submicron matrices (SMMs) as an intravaginal drug delivery system capable of delivering an anti-HIV-1 agent (zidovudine; AZT) over a prolonged duration. A three factor and three level (3³) Box-Behnken statistical design was employed to optimize the SMMs. Optimized PEG-encl-PEC:MUC SMMs prepared as a stable W/O emulsion (determined by the degree of reversible colloidal phenomena) were spherical with a mean particle size of 270.6 ± 5.533 nm and mean zeta potential of −34.4 ± 0.539 mV. The microencapsulation of AZT and the hydrogen bonding mediated shielding of AZT by SMMs was confirmed by Fourier Transform Infrared (FTIR) analysis. The thermochemical (differential scanning calorimetry and thermogravimetric analysis) data proposed that Ca²⁺-based macromolecular ionic crosslinking as well as the intermolecular interactions may be responsible for the thermal stability of the delivery system. The partially amorphous nature of drug-loaded SMMs, as confirmed by X-ray diffraction patterns, further strengthened the matricization of AZT into the pectin-mucin matrix. In vitro drug release studies from the SMMs showed approximately 91% zidovudine release in simulated vaginal fluid (SVF) and 94% in phosphate buffered saline (PBS) in 24 h. The mean dissolution time (MDT) of zidovudine from the SMMs was 5.974 h. The attainment of required dimensional structure and drug release profiles from SMMs highlights the potential of their inclusion into a secondary carrier system for extended and controlled intravaginal stay.