Self-assembled dipeptide nanospheres as single component based delivery vehicle for ampicillin and doxorubicin

Abstract

Effective delivery of therapeutic agents encounters many challenges such as uncontrolled drug release, low bioavailability of drugs, degradation of drugs in the intestinal transit and non-biocompatibility of the delivery vehicle. Thus, in the quest for advance drug delivery system, self-assembled dipeptide (Fmoc-L-Trp-L-Phe-OCH3) nanospheres (SPNS) were generated in aqueous medium with size ranging between 100 and 400 nm. The SPNS were examined for the presence of hydrophobic and hydrophilic domains which was followed by drug loading analysis (ampicillin and doxorubicin) into SPNS using HPLC. Further, SPNS demonstrated pH triggered morphological alterations leading to controlled release of loaded therapeutics. Additionally, SPNS exhibited low cytotoxicity and exceptional stability against enzymatic degradation. The system was further analyzed for in vitro cellular internalization of therapeutics. Thus, outcome of this analysis indicated that SPNS acts as single component, multifunctional drug delivery vehicle by addressing critical issues such as effective drug loading, pH responsive controlled release, biocompatibility, and stability against enzymatic degradation.