Novel Multifunctional Biocompatible Gelatin-Oleic Acid Conjugate: Self-Assembled Nanoparticles for Drug Delivery

Abstract

In this work, a novel, biocompatible conjugates of gelatin and oleic acid (GOC) were synthesized by a novel aqueous solvent-based method that overcame challenges of completely contrary solubility between gelatin and oleic acid (OA). The GO nanoparticles (GONs) and Paclitaxel encapsulated nanoparticles (PTX-GON) were prepared by self-assembly in water. These nanoparticles (NPs) were then conjugated with folic acid (FA) for targeting cervical cancer cells (Hela cells) and were characterized for their various physicochemical and pharmaceutical properties. Fourier transform infrared spectroscopy (FT-IR) and 1H NMR studies indicated the successful synthesis of GOC which showed low critical aggregation concentration in water (0.015 mg/ml). All NPs were stable in human blood serum and their mean diameters were below 300 nm suitable for passive targeting. Powder X-ray diffraction (PXRD) diffractograms showed the reduction in drug crystallinity and hence, leading to the solubility enhancement of PTX. The release of PTX from both PTX-GON and FA conjugated PTX-GON (PTX-FA-GON) was controlled for a long time. The cytotoxicity results demonstrated great advantages of PTX-FA-GON and PTX-GON over the conventional dosage form of pacliaxel (Taxol). These results, therefore, indicate that GOC is a promising material to prepare drug encapsulated NP as a controlled delivery system and PTX-FA-GON is a potential targeted delivery system for cancer therapy.

Folate and CD44 Receptors Dual-Targeting Hydrophobized Hyaluronic Acid Paclitaxel-Loaded Polymeric Micelles for Overcoming Multidrug Resistance and Improving Tumor Distribution

“…To date, it has been reported that polymeric micelles‐based drug delivery systems could have the potential to bypass P‐gp efflux via endocytosis mechanism, and have shown improved anticancer efficacy by tumor targeting . In addition, the receptor‐targeting nanocarriers provide an innovative alternative strategy for efficient intracellular uptake to overcome MDR effect and for tumor active targeting performance . In our study, the ability of a novel dual receptor‐targeting FA‐HA‐C 18 micelle to overcome P‐gp‐mediated drug resistance was investigated, and the tumor tissue targeting efficacy was evaluated.…”

“…18,19 In addition, the receptor-targeting nanocarriers provide an innovative alternative strategy for efficient intracellular uptake to overcome MDR effect and for tumor active targeting performance. 20 In our study, the ability of a novel dual receptor-targeting FA-HA-C 18 micelle to overcome P-gp-mediated drug resistance was investigated, and the tumor tissue targeting efficacy was evaluated.…”

The application of self-assembled nanostructures in peptide-based subunit vaccine development

“…Incorporating a self-assembly process in the production of drug or vaccine constructs offers several advantages. Firstly, the properties (for instance size, composition and charges) of the nanostructure itself can be precisely defined and have high batch-tobatch consistency [68]. Well-defined physical and chemical properties are crucial for any biomedical application of nanostructures.…”

Self-assembling polymer systems for advanced treatment of cancer and inflammation

“…A c c e p t e d M a n u s c r i p t method that overcame the opposite solubility between gelatin and oleic acid [125]. Gelatin was conjugated with high contents of cholesterol using N,N'--disuccinimidyl carbonate.…”

“…All NP were stable in human blood serum and their average size was below 300 nm, suitable for passive targeting.The release of PTX from both plain PTX--and FA conjugated PTX--loaded NP was controlled for a long time. The cytotoxicity results demonstrated great advantages of PTX--loaded NP either conjugated or not with FA, over the conventional dosage form of PTX (Taxol®)[125].Wareechuensook et al[126] modified gelatin into an amphiphilic molecule via conjugation…”