Retrovirus Drugs-Loaded PEGylated PAMAM for Prolonging Drug Release and Enhancing Efficiency in HIV Treatment.
Thi Thinh NguyenBao Phu NguyenDinh Tien Dung NguyenNgoc Hoi NguyenNguyen Dai HaiCuu Khoa NguyenPublished in: Polymers (2021)
Polyamidoamine dendrimer (PAMAM) with its unique characteristics emerges as a potential drug delivery system which can prolong releasing time, reduce the side effects but still retaining treatment efficiency. In this study, methoxy polyethylene glycol modified PAMAM generation 3.0 (G3.0@mPEG) is prepared and characterized via 1 H-NMR, FT-IR, and TEM. Subsequently, two antiretroviral agents (ARV) including lamivudine (3TC) and zidovudine (AZT) are individually encapsulated into G3.0@mPEG. The drug-loading efficiency, drug release profile, cytotoxicity and anti-HIV activity are then evaluated. The results illustrate that G3.0@mPEG particles are spherical with a size of 34.5 ± 0.2 nm and a drug loading content of about 9%. Both G3.0@mPEG and ARV@G3.0@mPEG show no cytotoxicity on BJ cells, and G3.0@mPEG loading 3TC and AZT performs sustained drug release behavior which is best fitted with the Korsmeyer-Peppas model. Finally, the anti-HIV activity of ARV via Enzymatic Assay of Pepsin is retained after being loaded into the G3.0@mPEG, in which about 36% of pepsin activity was inhibited by AZT at the concentration of 0.226 mM. Overall, PAMAM G3.0@mPEG is a promising nanocarrier system for loading ARV in HIV treatment and prevention.
Keyphrases
- drug release
- drug delivery
- hiv positive
- hiv infected
- antiretroviral therapy
- human immunodeficiency virus
- hiv testing
- hiv aids
- hepatitis c virus
- men who have sex with men
- hiv infected patients
- emergency department
- magnetic resonance
- induced apoptosis
- south africa
- combination therapy
- nitric oxide
- high throughput
- hydrogen peroxide
- cell cycle arrest
- wound healing