Development of a docetaxel micellar formulation using poly(ethylene glycol)–polylactide–poly(ethylene glycol) (PEG–PLA–PEG) with successful reconstitution for tumor targeted drug delivery

Abstract

Docetaxel (DTX)-loaded polymeric micelles (DTBM) were formulated using the triblock copolymer, poly(ethylene glycol)–polylactide–poly(ethylene glycol) (PEG–PLA–PEG), to comprehensively study their pharmaceutical application as anticancer nanomedicine. DTBM showed a stable formulation of anticancer nanomedicine that could be reconstituted after lyophilization (DTBM-R) in the presence of PEG 2000 and D-mannitol (Man) as surfactant and protectant, respectively. DTBM-R showed a particle size less than 150 nm and greater than 90% of DTX recovery after reconstitution. The robustly formed micelles might minimize systemic toxicity due to their sustained drug release and also maximize antitumor efficacy through increased accumulation and release of DTX from the micelles. From the pharmaceutical development point of view, DTBM-R showing successful reconstitution could be considered as a potent nanomedicine for tumor treatment.

Keywords:

• Nanomedicine
• lyophilization
• cancer
• reconstitution
• polymeric micelle

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This research was supported by a grant [16173MFDS542] from the Ministry of Food and Drug Safety in 2018 and by a National Research Foundation of Korea (NRF) grant funded by the Korean government (MSIP) [NRF- 2015R1A5A1008958].