Targeting efficacy and anticancer activity of polymeric nanoparticles of SN-38 on colon cancer cell lines

Abstract

Background Colorectal cancer is the third most prevailing cancer in the whole world. Chemotherapeutic agents which are used for treatment have severe side effects and also have unwanted exposure to healthy cells. In the present study, polymeric nanoparticles of SN-38 were prepared (using cationic and anionic polymers). They were optimized by Box Behnken design and characterized for its physicochemical properties and in vitro drug release. Optimized formulation (CsENP) was evaluated for its targeting efficacy by Gamma Scintigraphy studies on Swiss Albino mice and in vitro Cytotoxic assay against colon cancer cell line, viz. HT-29. Results The images of Whole body gamma scintigraphy imaging of Swiss Albino mice show that CsENP remained intact till 2 h and after that at 4 h imaging it started dispersing and releasing drug which continued till 20 h. In Organ distribution studies, no radioactivity was traced in heart from the formulation. Even in liver, spleen, kidney and lung trace radioactivity was seen after 6 h. In case of CsENP radioactivity was seen in small intestine after 2 h and maximum (87.8% radioactivity) is seen in colon and rectum area after 4 h. At equivalent concentrations, the in vitro cell viability of HT-29 cells after 72 h incubation time showed that CsENP have enhanced cytotoxicity. Conclusions The results obtained of Whole body gamma scintigraphy imaging and organ distribution of Swiss Albino mice show that CsENP is Colon targeting and was found to be effective against colon cancer cell lines.

Computational Amendment of Parenteral In Situ Forming Particulates’ Characteristics: Design of Experiment and PBPK Physiological Modeling

“…Recently, the development of injectable lipid and/or polymer-based particles with biodegradable as well as biocompatible characteristics, exhibiting optimal sizes ranging from 250 nm to 125 nm, has received attention. These particles are used to avoid the discomfort associated with surgical procedures for inserting bulky implants [8]. The latest research focuses on the preparation of a liquid lipid and/or polymer-based formulae containing the drug that solidifies and forms an implant at the site of injection upon contact with body fluids, which represents an effective substitute for conventional solid implants [9].…”