MPEG–PCL copolymeric nanoparticles in drug delivery systems

Figures & data

Figure 1. Schematic synthesis route of mPEG–PCL copolymer.

Figure 2. Schematic illustration of preparation of mPEG–PCL nanoparticles; (a) o/w emulsion solvent evaporation.

Figure 3. Schematic illustration of preparation of mPEG–PCL nanoparticles; (a) Nanoprecipitation.

Table 1. Categorization of demonstrated mPEG–PCL nanoparticles based on the method of preparation

Drug used	Objective of study	Brief method and outcome	References
Levonorgestrel	Modulation of release pattern by polymer modification	PCL–PEO–PCL microspheres (3–35 μm) of levo–norgestrel prepared using Tween-60 and PVA as stabilizer. An increase in PEO increased hydrophilicity, hence resulted in increased particle size distribution and decreased EE. The biphasic release pattern in the burst release phase (20% in 24 h) was found to be independent of polymer composition	Li, Cai, Bei, and Wang (2003)
Hot melt technique Estradiol	Study of suitability of copolymers for this technique	Estradiol containing methoxy–PEG (mPEG)–PCL oligomer microspheres were prepared by quenching the dispersion followed by freeze drying that produced a shell of PEG over PCL. The particle size, EE (46–78%), and DL efficiency (0.59–0.68) were reported to increase when PCL ratio was increased which in turn affected the drug release	Lee, Oh, Joo, and Jeong (2008)
o/w emulsion solvent evaporation Tetradrine	Improved efficacy and Development of histoculture drug response assay (HDRA)as a method to evaluate drug sensitivity	Physiochemical traits, cellular uptake, and cytotoxicity (in LoVo cells) and anti-tumor activity (HDRA) of tetradrine-loaded NPs prepared using mPEG–PCL and PEG–PCL–PEG were studied. NPs showed increased anti-tumor activity than free tetradrine. HDRA was reported to be a potential model for evaluation of anti-tumor potency	Choi, Ruktanonchai, Soottitantawat, and Min (2009)
Curcumin	Nanoprecipitation	Curcumin was encapsulated within monomethoxy poly(ethylene glycol)–poly(ε-caprolactone) (mPEG–PCL) micelles through a single-step nanoprecipitation method, leading to creation of curcumin-loaded mPEG–PCL (Cur-mPEG–PCL) micelles	Danafar, Rostamizadeh, Davaran, Valizadeh, et al. (2014)
Diffusion (solvent evaporation Tamoxifen	Targeted and controlled drug delivery	Tamoxifen-loaded PCL-NPs of size 250–300 nm with zeta potential of 25 mV, 64% EE for selective estrogen receptor modulation were prepared. Forty percent of drug was released in vitro within the first hour and the drug release continued up to 24 h	Chawla and Amiji (2002)
Human dermal broblast (HDF)	Effect of pore size and polymer composition tissue growth	The crystallinity of PCL–PEO fibers was increased after immersion in water in contrast to unaltered in case of PCL alone. Perfusion-seeded HDF in these scaffolds of different pore diameters greater than 6 μm were shown a faster growth after 21 days (49)	Lowery, Datta, and Rutledge (2009)
Paclitaxel [PCL-b–mPEG–Folate]	Design of micelles for improved activity and reduced toxicity	Folate–mPEG-b–PCL copolymeric micelles were of 150 nm and 50–130 nm with and without paclitaxel, respectively. The zero-order release pattern of folate–mPEG-b–PCL reported to show higher cytotoxicity in MCF-7 and HeLa cells than micelles without folate group	Park, Kim, Lee, and Lee (2005)
Doxorubicin (DOX) [PCL–PEG]	Vesicular carrier for controlled release	Loading of DOX into PCL–PEG micellar vesicles of 100 nm was comparable to liposomes. The dissolution rate increased with increase in hydrophilic portion of the copolymer, whereas PCL stabilized the membrane. The vesicles were resistant to destabilizing agents and released DOX in first-order pattern	Ahmed and Discher (2004)

Figure 4. AFM image of micelles.

Source: Kheiri et al. (2016).

Figure 5. Particle size distribution of mPEG–PCL–DOX micelles.

Figure 6. FTIR spectra of (a) curcumin, (b) mPEG–PCL and, (c) CUR-mPEG–PCL micelles.

Note: Spectrum blue is for curcumin, the red belongs to mPEG-PCL and pink belong to micelles. Source: Danafar, Rostamizadeh, Davaran, Valizadeh, et al. (2014).

Figure 7. The release profiles of curcumin from CUR-mPEG–PCL micelles in different release media (a) pH 7.4, (b) plasma, and (c) pH 5.5.

Source: Danafar, Rostamizadeh, Davaran, Valizadeh, et al. (2014).

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