Abstract
Study background: Acquired immunodeficiency syndrome (AIDS) is a severe disease of immune system caused by Human Immunodeficiency Virus (HIV). Zidovudine (AZT) is an effective antiretroviral drug against HIV. Due to its poor bioavailability (50-60%) and short elimination half life (0.5-3 h), frequent administration of zidovudine is required resulting into dose dependent hematological toxicity. In the present study, an attempt was made to develop sustained release formulation of AZT employing the poly (propyl ether imine) (PETIM) dendrimer as a carrier. Methods: The AZT-dendrimer complex was prepared and studied by Fourier transform infrared (FTIR) analysis and nuclear magnetic resonance (NMR) spectroscopy. The entrapment efficiency and in-vitro drug release studies were conducted by dialysis bag method. Hemolytic toxicity, pharmacokinetic and biodistribution studies were performed to evaluate the biosafety and sustained release characteristic of prepared formulation. Results and Conclusion: The cumulative amount of zidovudine released in 1 h from the AZT-dendrimer formulation was 6.5 ± 0.3 % compared with 95.8 ± 4.1% from the control drug solution. Zidovudine release was prolonged upto 14 h with zidovudine-dendrimer complex (94.3 ± 3.8%). The findings of present investigation illustrated that PETIM dendrimer effectively encapsulate AZT, and can be used as a biosafe carrier for sustained delivery of zidovudine.
Highlights
Acquired immunodeficiency syndrome (AIDS) is a disease of the human immune system caused by infection with human Immunodeficiency Virus (HIV) [1]
The cumulative amount of zidovudine released in 1 h from the AZT-dendrimer formulation was 6.5 ± 0.3 % compared with 95.8 ± 4.1% from the control drug solution
The prepared AZT-dendrimer complex was characterized by determining the IR and nuclear magnetic resonance (NMR) spectra of AZT, propyl ether imine (PETIM) dendrimer alone and AZT-dendrimer complex, as shown in Figures 2A-2C and 3A3C
Summary
Acquired immunodeficiency syndrome (AIDS) is a disease of the human immune system caused by infection with human Immunodeficiency Virus (HIV) [1]. Since the early reports of AIDS epidemic, it has become a harrowing disease which has spread like a plague. According to UNAIDS, 1.6 million people died globally in 2012 due to AIDS, while 35.3 million people are living with HIV out of which 2.3 million cases alone appeared in 2012 [2]. These alarming figures are sufficient to depict the challenges associated with the cure and prevention of the disease. Still no single drug or method is available which can completely eradicate the HIV and cure the AIDS. Number of policies has appeared like Millennium Development Goal (MDG 6), National HIV/AIDS Strategy (NHAS), International HIV/ AIDS Alliance and presently, lot is being done to manage AIDS which resulted in significant reduction in the number AIDS cases over the past few years
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