Abstract
Objective: The present investigation aimed to develop and characterize Eudragit S-100 coated alginate beads bearing oxaliplatin loaded liposomes for colon-specific drug delivery. Methods: Liposomes were formulated by the thin-film hydration method. The process and formulation variables were optimized by Box-Behnken design (BBD) with the help of Design-Expert® Software. Three independent variables taken were HSPC: Chol molar ratio (X1), hydration time (X2), and sonication time (X3). The response variables selected were entrapment efficiency of oxaliplatin, polydispersity index, and vesicle size. Results: The liposomes possessed an average vesicle size of 110.1±2.8 nm, PDI 0.096±0.3, zeta potential of-6.70±1.4 mV, and entrapment efficiency of 27.65%. The beads were characterized for their size, in vitro drug release, and swelling index. The degree of swelling of the beads was found to be 2.3 fold higher at pH 7.4 than at pH 1.2. The in vitro drug release depicted a sustained drug release in 48 h. Conclusion: The outcomes of the study proposed that the developed system can be effectively used for site-specific drug delivery to the colon via the oral route.
Highlights
Colorectal cancer (CRC) originates from the inner wall of the colon epithelium
The developed liposomes were investigated for dependent variables like %EE of OHP (Y1), polydispersity index (PDI) (Y2), and vesicle size (Y3) on the chosen independent variables, Hydrogenated soy phosphatidylcholine (HSPC): Chol molar ratio (X1), hydration time (X2), and sonication time (X3) as per Box-Behnken design (BBD)
The Box-Behnken design was applied for the optimization of formulation and process parameters, namely the molar ratio of HSPC: Chol, Hydration time, and sonication time
Summary
Colorectal cancer (CRC) originates from the inner wall of the colon epithelium. Despite the advancements in its diagnostic methods, it is fatal It is marked by the development of colorectal polyps, which are abnormal growths in the intestinal lining. OHP is a third-generation platinum chemotherapeutic drug that can form Pt-DNA adducts with DNA chains to produce inter-chain crosslinking and intra-chain cross-linking, resulting in DNA damage [3, 4]. It can inhibit the synthesis of DNA and RNA, and trigger systemic immune reactions, leading to apoptosis [5]
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