Micelles of Methoxy Poly(ethylene glycol)–Poly(ε-caprolactone) as a Novel Drug Delivery Vehicle for Tacrolimus

Abstract

As a traditional immunosuppressive drug, tacrolimus showed the potency in treating ulcerative colitis. In this study, a novel drug delivery vehicle achieved by self-assembly was applied to tacrolimus. During the preparation, amphiphilic copolymer MPEG-PCL was chosen to form the unique core-shell structure, and tacrolimus was loaded into the hydrophobic core due to its great hydrophobicity. After several relevant tests, MPEG-PCL (2000-2000) was selected to be the most suitable and safest copolymer for drug carrier. For the tacrolimus loaded MPEG-PCL (2000-2000) micelles, the mean particle size and drug entrapment efficiency were ca. 25 +/- 5 nm and 98.47 +/- 0.43% respectively. The micelles could be stored for quite a long time even at room temperature after freeze-drying, and the freeze-drying process didn't affect the monodispersity of micelles. Transmission electron microscope (TEM) image emerged the spherical shape of micelles. Both Differential Scanning Calorimetric (DSC) and X-ray Diffractometer (XRD) assays demonstrated that tacrolimus was relatively completely incorporated into the core-shell structure. In vitro release profiles showed the apparent sustained release behavior compared with tacrolimus solution. Above all, animal treatment showed the most satisfactory therapeutic effect of tacrolimus loaded micelles, which means the micelles possess the ability to treat ulcerative colitis induced by dextran sulfate sodium (DSS) in mice. Therefore, micelles of MPEG-PCL could be a very promising novel vehicle for tacrolimus.

Long-Term Evaluation of Dip-Coated PCL-Blend-PEG Coatings in Simulated Conditions

“…Therefore, in this study, we propose a combination of PCL and the soluble polyethylene glycol (PEG), a polymer reputed for its biocompatibility, tissue reaction, and biodegradation kinetics [19], and, respectively, for its hydrophilicity, nontoxicity, nonimmunogenicity and absence of antigenicity [9,20,21]. The PEG-based materials designed for biomedical applications include scaffolds [22], micelles [23], nanoparticles [24], and coatings [25].…”

Olaparib nanoparticles potentiated radiosensitization effects on lung cancer

“…Ola presents with a series of physicochemical properties, such as poor solubility, low bioavailability, and an extensive range of tissue toxicity that largely offset the use and therapeutic benefits of Ola. In our previous study, we demonstrated that MPEG-PCL nanoparticles were outstanding carriers for hydrophobic drugs in virtue of the hydrophilic Time (days) Body weight (g) 28 34 PEG segment being introduced into PCL backbones. [25][26][27][28] Therefore, in our study, MPEG-PCL was used as a carrier to prepare Ola-NPs.…”

Novel pH-sensitive hydrogels for 5-aminosalicylic acid colon targeting delivery:in vivostudy with ulcerative colitis targeting therapy in mice

“…The animals were sacrificed 24 h after the last drug loaded hydrogels administration. Their distal colons were resected and collected (Wang et al, 2012). Specimens were taken from the collected colon, and then, the specimens were fixed in neutral formalin and embedded in paraffin.…”