Renewable poly(δ-decalactone) based block copolymer micelles as drug delivery vehicle: in vitro and in vivo evaluation

Saudi Pharmaceutical Journal

Jitendra Gupta¹  Ari Rosling²  Jessica M. Rosenholm³  Kuldeep K. Bansal⁴ 

[1] Institute of Pharmaceutical Research, GLA University, Mathura, Uttar Pradesh 281406, India;Laboratory of Polymer Technology, Centre of Excellence in Functional Materials at Biological Interfaces, Åbo Akademi University, Biskopsgatan 8, 20500 Turku, Finland;Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Abo Akademi University, 20520 Turku, Finland;School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, United Kingdom;

关键词: Biodegradable polymers;    Controlled release;    Micelles;    Polymeric drug carrier;    Toxicity;    Bioavailability;   

DOI  :  10.1016/j.jsps.2018.01.006

来源: DOAJ

【 摘 要 】

Polymers from natural resources are attracting much attention in various fields including drug delivery as green alternatives to fossil fuel based polymers. In this quest, novel block copolymers based on renewable poly(δ-decalactone) (PDL) were evaluated for their drug delivery capabilities and compared with a fossil fuel based polymer i.e. methoxy-poly(ethylene glycol)-b-poly(ε-caprolactone) (mPEG-b-PCL). Using curcumin as a hydrophobic drug model, micelles of PDL block copolymers with different orientation i.e. AB (mPEG-b-PDL), ABA (PDL-b-PEG-b-PDL), ABC (mPEG-b-PDL-b-poly(pentadecalactone) and (mPEG-b-PCL) were prepared by nanoprecipitation method. The size, drug loading and curcumin stability studies results indicated that mPEG-b-PDL micelles was comparable to its counterpart mPEG-b-PCL micelles towards improved delivery of curcumin. Therefore, mixed micelles using these two copolymers were also evaluated to see any change in size, loading and drug release. Drug release studies proposed that sustained release can be obtained using poly(pentadecalactone) as crystalline core whereas rapid release can be achieved using amorphous PDL core. Further, mPEG-b-PDL micelles were found to be non-haemolytic, up to the concentration of 40 mg/mL. In vivo toxicity studies on rats advised low-toxic behaviour of these micelles up to 400 mg/kg dose, as evident by histopathological and biochemical analysis. In summary, it is anticipated that mPEG-b-PDL block copolymer micelles could serve as a renewable alternative for mPEG-b-PCL copolymers in drug delivery applications.

【 授权许可】

Unknown