Electrospun Amorphous Solid Dispersions with Lopinavir and Ritonavir for Improved Solubility and Dissolution Rate

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Lopinavir (LPV) and ritonavir (RTV) are crucial antiretroviral drugs with poor solubility, limiting their bioavailability.
• Amorphous solid dispersions (ASDs) are a key strategy to enhance the solubility and dissolution rates of poorly soluble active pharmaceutical ingredients (APIs).

Purpose of the Study:

• To develop novel amorphous solid dispersions (ASDs) of lopinavir (LPV) and ritonavir (RTV) using the electrospinning technique.
• To investigate the impact of different polymeric carriers (PVP, KVA, Eudragit E100) and drug content on the amorphization and properties of LPV and RTV ASDs.

Main Methods:

• Electrospinning was employed to fabricate drug-loaded fibers containing LPV and RTV with various polymeric carriers.
• Characterization involved microscopy, Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), wettability assessment, and dissolution studies.

Main Results:

• Electrospinning achieved complete amorphization of both LPV and RTV, irrespective of the polymer matrix or drug loading.
• Specific polymer combinations, Eudragit E100 for LPV and KVA for RTV, improved equilibrium solubility and dissolution rates, even with a beads-on-string morphology.
• The electrospinning process demonstrated effectiveness in creating ASDs for poorly soluble APIs.

Conclusions:

• Electrospinning is a viable technique for producing amorphous solid dispersions (ASDs) of poorly soluble antiretroviral drugs like lopinavir and ritonavir.
• The choice of polymeric carrier significantly influences the solubility and dissolution performance of the resulting ASDs.
• This study presents a novel approach for enhancing the delivery of essential antiretroviral agents.