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AAPS PharmSciTech. 2018 Oct;19(7):3110-3122. doi: 10.1208/s12249-018-1132-y. Epub 2018 Aug 15.

Strategic Pentablock Copolymer Nanomicellar Formulation for Paclitaxel Delivery System.

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University of Missouri-Kansas City, Kansas City, Missouri, USA.
University of Missouri-Kansas City, Kansas City, Missouri, USA.


Nanomicelles (NM) enhance solubility and absorption of active pharmaceutical ingredients (APIs). Various polymers and non-polymers are utilized to prepare nanomicellar formulations to achieve high absorption and delivery of drugs. The main purpose of this study was to develop drug-loaded nanomicelles with pentablock copolymers for paclitaxel delivery. Monomers of lactide, ε-caprolactone, and polyethylene-glycol were utilized to prepare pentablock copolymer by ring opening technique. The pentablock nanomicelles (PBNM) were formulated by evaporation and rehydration. Both copolymers and nanomicelles were analyzed by H-NMR, FTIR, and XRD. Nanomicelles were further analyzed for size and zeta potential using dynamic light scattering (DLS) and by H-NMR and TEM. The XRD, FTIR, and H-NMR analyses confirmed the structures of the pentablock copolymers. Average size was 20 nm ± 5.00 nm, and ζ-potential is around zero. H-NMR and FTIR analyses for Paclitaxel-PBNM indicated peaks of paclitaxel and the polymer, confirming successful encapsulation. TEM showed spherical morphology and size range similar to that obtained by DLS. In vitro release studies revealed slow first-order paclitaxel release rate from pentablock nanomicelles in phosphate buffer solution (PBS). Confocal laser scanning microscopy analysis with coumarin-6-loaded in PBNM indicated that pentablock nanomicelles were efficiently taken into prostate cancer (PC-3) cells. Cell proliferation assay showed that nanomicelles were able to ferry adequate amounts of paclitaxel drug into PC-3 cells and subsequently inhibiting PC-3 cell proliferation significantly. Results confirmed that pentablock copolymer can generate drug-loaded nanomicelles with desirable sizes and zeta potential. These demonstrate potentiality of pentablock nanomicelles as carrier for anticancer delivery.


coumarin-6; nanomicellar formulation; paclitaxel delivery; pentablock copolymers; prostate cancer

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