Development of lapatinib nanosponges for enhancing bioavailability

• Published in: Journal of drug delivery science and technology 2021-10, Vol.65, p.102684, Article 102684
• Main Authors: Prabhu, Pavithra P., Prathvi, Gujaran, Tanvi V., Mehta, Chetan H., Suresh, Akhil, Koteshwara, K.B., Pai, K Girish, Nayak, Usha Y.
• Format: Article
• Language: English
• Subjects: Emulsion solvent diffusion method; In vitro dissolution studies; In vivo pharmacokinetics studies; Lapatinib; Nanosponges; Solubility enhancement
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2021.102684

The present study is aimed to formulate lapatinib nanosponges (LPT NSs) to enhance its aqueous solubility and bioavailability. LPT loaded NSs were fabricated using Eudragit RS100 as polymer and polyvinyl alcohol as a stabilizer. The optimized formulation was evaluated for morphological characterization, solid-state characterization, accelerated stability studies, in vitro release studies and in vivo pharmacokinetic studies. Solid-state characterization such as Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) studies showed the retention of drug characteristics peaks in the formulation which indicates no or negligible chemical interactions between the LPT and excipients used for the formulation preparation. Morphological characterization such as Atomic Force Microscopy (AFM) and Field Emission Scanning Electron Microscopy (FESEM) confirmed the formation of nanosponges with porous structures. Saturation solubility studies and in vitro dissolution studies proved the enhancement of aqueous solubility as well as dissolution rate of LPT in the form of NSs as compared to pure form of LPT in the basic medium as compared to the acidic medium. Also, in vivo pharmacokinetic study proved significant improvement in AUC and Cmax of the LPT NSs when compared to the pure LPT. Thus LPT-loaded NSs are proven to have high bioavailability and potential scope to reduce the oral dose of LPT by preparing the NSs. [Display omitted]