Abstract
Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.
Highlights
Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses
in situ self-assembly nanoparticles (ISNPs) were monodispersed with a narrow size distribution indicated by a polydispersity index (P.I.) of less than 0.35 (Figure 2)
The stability of particle size during storage is of less concern for the ISNP-based injection, because the mixture of drugs with lipid and surfactant is the final formulation that is kept on the shelf, and the ISNPs form after injection
Summary
Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. The ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies. Human immunodeficiency virus (HIV) is a major global public health issue, with approximately 34.7 million people living with it, 690,000 people having died from related illnesses, and 1.7 million people being newly infected worldwide in 2019, according to the. There is currently no cure for HIV infection It can be treated and prevented by using oral HIV medications called antiretroviral therapy (ART). Even though medications can improve the survival of patients infected with HIV, there are adherence issues, such as forgetting to take HIV medications, dosing complexity, side effects, and pill burden [2,3,4], and at least 95% adherence is necessary for effective HIV viral suppression [5]
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