[Tetrandrine loaded sustained-release microcapsules for lung targeting]

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Biomaterials

Context:

• Pulmonary hypertension (PH) poses a significant therapeutic challenge.
• Tetrandrine (TET) exhibits anti-PH properties but suffers from toxicity and suboptimal delivery.
• Targeted drug delivery systems are crucial for enhancing therapeutic efficacy and minimizing side effects.

Purpose:

• To develop a lung-targeted, sustained-release drug delivery system for tetrandrine (TET) using albumin microencapsulation.
• To evaluate the physicochemical properties, in vitro release kinetics, and in vivo biodistribution of TET-loaded microcapsules.
• To assess the anti-pulmonary hypertension efficacy and toxicity profile of the developed microcapsules.

Summary:

• Albumin microcapsules loaded with tetrandrine (TET) were successfully prepared using a novel spray drying-thermal denaturation technique.
• The microcapsules exhibited desirable characteristics, including high drug loading (37.88%) and significantly reduced in vitro drug release rates.
• In vivo studies demonstrated enhanced lung targeting, with higher TET concentrations and prolonged retention time in mouse lungs compared to conventional TET injection.
• A strong in vitro-in vivo correlation was established, validating the predictive capability of the release studies.

Impact:

• The developed microencapsulation technique offers a promising method for creating sustained-release drug delivery systems.
• The lung-targeted TET-loaded albumin microcapsules show potential for low-toxicity, high-efficacy treatment of pulmonary hypertension.
• This approach could lead to improved therapeutic strategies for lung diseases requiring targeted drug delivery.