The aim of the study was to prepare and characterize the nanosize drug loaded bio-flexi films using the novel bioexcipient isolated from the fresh leaves of the piper betle (bioexcipient P) and to explore the potentiality of the lip skin as a novel transvermillion drug delivery system. The bioexcipient prepared using a simplified economical process and was subjected to various physiochemical evaluations along with the spectral analysis including UV, FT-IR, SEM, Mass and 1H NMR. The nanosized bioflexi film formulated with the novel bioexcipient was screened for its functional properties, such as including filmability. Nanosized olanzapine loaded bioflexi films were formulated by using bioexcipient P as a film former and dextrose as a flexicizer. The formulated nanosized bioflexi films were subjected to various tests such as evaluating the, thickness, folding endurance, swelling index and in vitro release. The size of the nanoparticle was found to be 100 nm. The release of the nanosized olanzapine was maintained over 48 h, which was confirmed in in vitro release experiment. The results revealed that this biopolymer had a promising filmability and bioadhesivity. The formulated nanosized bioflexi films are feasible for delivering the olanzapine by transvermillion administration and for drugs that undergo first-pass metabolism.