EGF‐functionalized lipid–polymer hybrid nanoparticles of 5‐fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma

Abstract

The present research work describes development of dual drug‐loaded lipid–polymer hybrid nanoparticles (LPHNPs) of anticancer therapeutics for the management of colon cancer. The epidermal growth factor (EGF)‐functionalized LPHNPs coloaded with 5‐fluorouracil (FU) and sulforaphane (SFN) were prepared by one‐step nanoprecipitation method. Box–Behnken design was applied for optimizing the material attributes and process parameters. The optimized LPHNPs revealed particle size 198 nm, polydispersity index 0.3, zeta potential −25.3 mV, and drug loading efficiency 19–20.3% for 5‐FU and SFN, respectively. EGF functionalization on LPHNPs was confirmed from positive magnitude of zeta potential to 21.3 mV as compared with the plain LPHNPs. In vitro drug release performance indicated sustained and non‐Fickian mechanism release nature of the drugs from LPHNPs. Anticancer activity evaluation in HCT‐15 colon cancer cells showed significant reduction (p < 0.001) in the cell growth and cytotoxicity of the investigated drugs from various treatments in the order: EGF‐functionalized LPHNPs > plain LPHNPs > free drug suspensions. Overall, the research work corroborated improved treatment efficacy of EGF‐functionalized LPHNPs for delivering chemotherapeutic agents for the management of colon carcinoma.

Baicalin-Loaded Lipid–Polymer Hybrid Nanoparticles Inhibiting the Proliferation of Human Colon Cancer: Pharmacokinetics and In Vivo Evaluation

“…To overcome the limitations of individual liposomes and polymeric nanoparticles (NPs), traditional lipid- and polymer-based nanoparticles have many drawbacks, including dose-related toxicity, poor selectivity, fast diffusion systemically, and short half-lives in the circulation [ 14 , 15 ]. To improve drug accumulation in the colon, lipid–polymer hybrid nanoparticles (LPHNPs) can be employed to circumvent the physiological and anatomical hurdles.…”

“…To improve drug accumulation in the colon, lipid–polymer hybrid nanoparticles (LPHNPs) can be employed to circumvent the physiological and anatomical hurdles. By wisely controlling the particle size around 0.23 µm, CRC may be targeted passively [ 14 ]. LPHNPs have emerged as a viable drug delivery technology.…”

“…LPHNPs have emerged as a viable drug delivery technology. LPHNPs encompass the benefits of both liposomes and nanoparticles, while overcoming their drawbacks [ 14 ]. Instead, a well-constructed hybrid nanoparticle will have a hydrophobic polymeric core to slow the release of water-soluble drugs and a biocompatible lipid shell to protect the core from the stoma environment [ 14 , 15 ].…”

“…LPHNPs encompass the benefits of both liposomes and nanoparticles, while overcoming their drawbacks [ 14 ]. Instead, a well-constructed hybrid nanoparticle will have a hydrophobic polymeric core to slow the release of water-soluble drugs and a biocompatible lipid shell to protect the core from the stoma environment [ 14 , 15 ]. Biocompatible, biodegradable, prolonged drug-release pattern, and enhanced loading-capacity-tailored drug delivery vehicles can improve chemotherapeutic effectiveness against specific cell types [ 14 , 15 ].…”

Co-delivery of sorafenib and metformin from amphiphilic polypeptide-based micelles for colon cancer treatment

“…The nanomaterials-based drug carriers not only protect the encapsulated agents during blood circulation but also increase the accumulation in the tumor site ( 11 ). Furthermore, co-drug-loaded nanoparticles to deliver combination therapy for CRC treatment have attracted more and more attention ( 12 ). Encapsulating chemotherapeutic agents with synergistic effects can increase the antitumor efficacy against CRC ( 13 ).…”