Pluronic F127 and D-α-Tocopheryl Polyethylene Glycol Succinate (TPGS) Mixed Micelles for Targeting Drug Delivery across The Blood Brain Barrier

Abstract

A novel polymeric mixed micelle composed of Pluronic F127 and D-α-tocopheryl polyethylene glycol succinate (TPGS) was developed to improve the delivery of fluorescent dyes and protein across the blood brain barrier (BBB). Rhodamine 123 (Rho123) and DiR loaded mixed micelles, composed of Pluronic F127 and TPGS with proportion of 4:1 (FT), were prepared by thin-film hydration, and β-galactosidase (β-Gal) loaded FT mixed micelles were prepared by self-assembly. The brain-targeted capability of FT mixed micelles were evaluated both in vitro and in vivo. The FT mixed micelles showed that a average particle size of 20.03 nm, and a low CMC of 0.0031% in water. The in vitro release of Rho123 from Rho123 loaded FT mixed micelles (FT/Rho123) presented a sustained-release property. FT/Rho123 also showed higher efficiency for the accumulation in brain capillary endothelial cells (BCECs) and brain tissues. β-Gal, a model protein, was also delivered and accumulated efficiently in the brain by spontaneous loading in the FT mixed micelles. Therefore, the results indicated that F127/TPGS mixed micelles may be considered as an effective nanocarrier for the brain-targeted delivery of diagnostic and therapeutic drugs.

Optimized vinpocetine-loaded vitamin E D-α-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies

“…TPGS has also been reported as a skin permeation enhancer. 39,40 ALA is a powerful antioxidant that could enhance the cognitive function in patients with Alzheimer's disease. ALA molecules act as surface active agents, reduce the surface energy, and spontaneously aggregate in aqueous medium to form micelles.…”

Safety and biocompatibility of injectable vaccine adjuvants composed of thermogelling block copolymer gels

“…[25][26][27] Our research group has previously synthesized a family of PBCs based on the amphiphilic Pluronic F127 triblock copolymer. [25][26][27] Our research group has previously synthesized a family of PBCs based on the amphiphilic Pluronic F127 triblock copolymer.…”

“…Biocompatible amphiphilic block copolymers based on Pluronic have been used in gene therapy and targeted drug delivery. [25][26][27] Our research group has previously synthesized a family of PBCs based on the amphiphilic Pluronic F127 triblock copolymer. 20 This family of PBCs differs in its cationic outer blocks and, therefore, in its pH-dependent micellization behavior, and its ability to form complexes with nucleic acids for gene delivery.…”

Synthesis and evaluation of hydrophobically modified fenugreek gum for potential hepatic drug delivery

“…A sharp cross-point was considered as CMC value by extrapolating the intensity ratio at low and high concentration regions to obtain two straight lines [26], and the CMC was found to be 0.042 mg/ml. The low CMC can ensure enhanced stability of FG-C 18 NMs in aqueous solution in vitro and in vivo after intravenous administration [27].…”