Sodium alginate/polyvinylpyrrolidone/lapatinib-loaded Zr–metal organic framework: biocompatibility evaluation and pH-responsive in vitro drug release for oral delivery applications

Abstract

Recent advancements in drug delivery systems have transformed drug administration methods to ensure precise, targeted delivery with minimal side effects. Innovations involving polymer–metal organic frameworks can significantly improve drug stability and controlled release properties. In this study, a drug delivery system based on a zirconium metal organic framework (Zr-MOF), sodium alginate (SA), and polyvinylpyrrolidone (PVP) was developed. Lapatinib, an oral anticancer drug used to treat breast cancer, was incorporated into the pores of a Zr–metal organic framework. Although lapatinib selectively inhibits HER2 receptors and cancer cell proliferation, it has limitations, primarily due to its poor oral bioavailability and side effects resulting from its toxicity. To address these issues, we embedded a drug-loaded Zr–metal organic framework in a sodium alginate (SA)/polyvinylpyrrolidone (PVP) polymer matrix. This combination has been proposed to modulate drug release characteristics, promote pH-responsive targeted drug delivery, increase stability, enhance mechanical properties (tensile strength of 6.5 MPa), improve hydrophilicity, and potentially enhance biocompatibility of the composites. In vitro release studies showed minimal lapatinib release (13%) over 48 h under simulated gastric conditions (pH 1.2), whereas drug release reached 91% at intestinal pH (6.8) during the same period. These findings indicate that the system can intrinsically prevent premature gastric release, emphasizing its potential to achieve high therapeutic effects at lower doses with reduced side effects. Biocompatibility assays indicated over 94% viability in the relevant cell lines after 24 and 48 h, indicating the favorable cytocompatibility of the composites. Overall, this composite platform provides controlled, sustained, and site-specific release of lapatinib, which could potentially enhance oral bioavailability, reduce dosage frequency, and systemic toxicity.