Anti-HIV type 1 Polyclonal antibody

This study was aimed at formulating Lopinavir loaded Vitamin E-TPGS micelles to enhance its oral bioavailability. Lopinavir is an HIV-1 protease inhibitor with low aqueous solubility leading to poor oral bioavailability and thus frequent dosing. Drug loaded micelles were fabricated using thin film hydration technique and optimized by two-factor five-level central composite design. For this purpose independent variables selected were TPGS to drug ratio and rotational speed of rotary evaporator, whereas dependent variables chosen were particle size and % entrapment efficiency. The effect of an independent variable on the dependent variable was studied by generating a quadratic polynomial model. Results of in vitro characterization showed that prepared lopinavir micelles exhibited particle size 91.71 nm, polydispersity index 0.129, zeta potential -24.8 mV, entrapment efficiency 99.36 +/- 1.06% and drug loading 20.83 +/- 1.23%. Results of DSC and P-XRD evaluation revealed that drugs were successfully encapsulated inside the Vitamin E-TPGS micelles. In vitro release studies displayed enhancement in drug dissolution as a result of its loading into micelles. TEM images showed that micelles were spherical. On oral administration of lopinavir micelles; the relative bioavailability was boosted by 3.17 folds compared to lopinavir suspensions. Thus, we can conclude that TPGS based micelles possess the prodigious potential to overcome the challenges of current HAART therapy.

The human immunodeficiency virus type 1 (HIV-1) is the major etiological agent responsible for the acquired immunodeficiency syndrome (AIDS), which is a serious infectious disease and remains one of the most prevalent problems at present. Currently, combined antiretroviral therapy is the primary modality for the treatment and management of HIV/AIDS, but the long-term use can result in major drawbacks such as the development of multidrug-resistant viruses and multiple side effects. 1,2,3-Triazole is the common framework in the development of new drugs, and its derivatives have the potential to inhibit various HIV-1 enzymes such as reverse transcriptase, integrase, and protease, consequently possessing a potential anti-HIV-1 activity. This review covers the recent advances regarding the 1,2,3-triazole hybrids with potential anti-HIV-1 activity; it focuses on the chemical structures, structure-activity relationship, and mechanisms of action, covering articles published from 2010 to 2020.