Abstract
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 1H-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.
Highlights
Retroviruses have been receiving a lot of attention due to their association with several serious illness such as cancers, acquired immunodeficiency syndrome (AIDS) and neurologic diseases
Dialysis membrane with molecular weight cut-off (MWCO) of 3.5 kDa was bought from Spectra/Por® (Texas City, TX, USA)
nitrophenyl chloroformate (NPC)-activated mPEG was conjugated on G3.0 surface to form G3.0@mPEG and release nitrophenol
Summary
Retroviruses (family Retroviridae) have been receiving a lot of attention due to their association with several serious illness such as cancers, acquired immunodeficiency syndrome (AIDS) and neurologic diseases. Retroviruses contain a diploid RNA genome as their genetic material and convert their RNA genome to double-stranded DNA after infecting the host cells. This dual genetic system allows retroviruses to transmit from cell to cell as packaged RNA but still leave a DNA copy in the infected cell to transmit from one cell generation to the [1]. To prevent the HIV/AIDS epidemic, antiretroviral drugs (ARV) including Lamivudine (3TC) and zidovudine (AZT) that work by inhibiting reverse transcription and disrupting the synthesis of DNA from viral RNA have been used [4,5,6].
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