Polymeric micelle as a nanocarrier for delivery of therapeutic agents: A comprehensive review
For selective and effective drug delivery of therapeutic agent nanocarriers are the most effective agents. Micelles are an aggregate of surfactant molecules that dispersed in a liquid colloid. Micelles have a variety of shapes such as spheres, rods, vesicles, tubules, and lamellae. The shape and size of a micelle are a function of the molecular geometry of its surfactant molecules and solution conditions such as surfactant concentration, temperature, pH, and ionic strength. Poly Ethylene Glycol (PEG) is the most commonly used hydrophilic segment of micelles for drug delivery. Besides PEG, other polymers including poly (N-vinyl pyrrolidone) (PVP) and poly (N-isopropyl acrylamide) (pNIPAM) have also been used as hydrophilic portion of micelles. In this review we all discus about the polymeric micelles (PMs) as a nanocarriers for delivery of therapeutic agents.
Keywords: Polymeric Micelles, Colloids, Nanocarriers, Drug Delivery, Poly Ethylene Glycol(PEG)
2. Gaucher G, Dufresne MH, Sant VP, Kang N, Maysinger D, Leroux JC. Block copolymer micelles: preparation, characterization and application in drug delivery. J Control Release. 2005; 109(1–3):169–88.
3. Sutton D, Nasongkla N, Blanco E, Gao J. Functionalized micellar systems for cancer targeted drug delivery. Pharm Res. 2007; 24(6):1029–46.
4. Rarokar NR, Khedekar PB, Formulation and evaluation of docetaxel trihydrate loaded self-assembled nanocarriers for treatment of HER2 positive breast cancer. Journal of drug delivery and Therapeutics. 2017; 7(6):1-6
5. Rarokar N. R., Khedekar P. B., Bharne A., Umekar M., Development of self-assembled nanocarriers to enhance antitumor efficacy of docetaxel trihydrate in MDA-MB-231 cell line, Int. J. Biol. Macromol. 125 (2019) 1056-1068. DOI:doi.org/10.1016/j.ijbiomac.2018.12.130
6. Choucair A, Eisenberg A. Control of amphiphilic block copolymer morphologies using solution conditions. Eur Phys J E Soft Matter. 2003; 10(1):37–44.
7. Yu Y, Zhang L, Eisenberg A. Morphogenic effect of solvent on crew-cut aggregates of amphiphilic diblock copolymers. Macromolecules. 1998; 31(4):1144–54.
8. Shen H, Zhang L, Eisenberg A. Multiple pH-induced morphological changes in aggregates of polystyrene-block-poly(4-vinylpyridine) in DMF/H2O mixtures. J Am Chem Soc. 1999; 121(12):2728–40.
9. Geng Y, Dalhaimer P, Cai S, Tsai R, Tewari M, Minko T, et al. Shape effects of filaments versus spherical particles in flow and drug delivery. Nat Nanotechnol. 2007; 2(4):249–55.
10. Benahmed A, Ranger M, Leroux JC. Novel polymeric micelles based on the amphiphilic diblock copolymer poly(N-vinyl-2- pyrrolidone)-block-poly(D, L-lactide). Pharm Res. 2001; 18(3):3238.
11. Chung JE, Yokoyama M, Aoyagi T, Sakurai Y, Okano T. Effect of molecular architecture of hydrophobically modified poly(Nisopropylacrylamide) on the formation of thermoresponsive core-shell micellar drug carriers. J Control Release. 1998; 53(1– 3):119–30.
12. Riess G., “Micellization of block copolymers,” Progress in Polymer Science, vol. 28, no. 7, pp. 1107–1170, 2003. View at Publisher • View at Google Scholar • View at Scopus
13. Jones M.-C. and J.-C. Leroux, “Polymeric micelles—a new generation of colloidal drug carriers,” European Journal of Pharmaceutics and Biopharmaceutics, vol. 48, no. 2, pp. 101–111, 1999. View at Publisher • View at Google Scholar • View at Scopus
14. Rarokar N.R., Saoji S.D., Khedekar P.B., Investigation of effectiveness of some extensively used polymers on thermoreversible properties of Pluronic® tri-block copolymers, J. Drug Delivery Sci. Technol. 44 (2018) 220–230. DOI:doi.org/10.1016/j.jddst.2017.12.002
15. Van Butsele K., Sibret P., Fustin C. A. et al., “Synthesis and pH-dependent micellization of diblock copolymer mixtures,” Journal of Colloid and Interface Science, vol. 329, no. 2, pp. 235–243, 2009. View at Publisher • View at Google Scholar • View at Scopus
16. Parajapati SK, Maurya SD, Das MK, Tilak VK, Verma KK, Dhakar RC, Potential application of dendrimers in drug delivery: A concise review and update, Journal of Drug Delivery and Therapeutics 2016; 6(2):71-88
17. Alakhov V. Y., Moskaleva E. Y., Batrakova E. V., and A. V. Kabanov, “Hypersensitization of multidrug resistant human ovarian carcinoma cells by pluronic P85 block copolymer,” Bioconjugate Chemistry, vol. 7, no. 2, pp. 209–216, 1996. View at Google Scholar • View at Scopus .
18. Rarokar N.R., S.D. Saoji, N.A. Raut, J.B. Taksande, P.B. Khedekar, V.S. Dave, Nanostructured cubosomes in a thermoresponsive depot system: an alternative approach for the controlled delivery of docetaxel, AAPS PharmSciTech 17 (2015) 436–445. DOI:10.1208/s12249-015-0369-y
19. Nishiyama N., Kataoka K., “Preparation and characterization of size-controlled polymeric micelle containing cis-dichlorodiammineplatinum(II) in the core,” Journal of Controlled Release, vol. 74, no. 1-3, pp. 83–94, 2001. View at Publisher • View at Google Scholar • View at Scopus
20. Y. Li and G. S. Kwon, “Methotrexate esters of poly(ethylene oxide)-block-poly(2-hydroxyethyl-L- aspartamide). Part I: effects of the level of methotrexate conjugation on the stability of micelles and on drug release,” Pharmaceutical Research, vol. 17, no. 5, pp. 607–611, 2000. View at Publisher • View at Google Scholar • View at Scopus .
21. Lavasanifar A., Samuel J., and G. S. Kwon, “Micelles self-assembled from poly(ethylene oxide)-block-poly(N-hexyl stearate L-aspartamide) by a solvent evaporation method: effect on the solubilization and haemolytic activity of amphotericin B,” Journal of Controlled Release, vol. 77, no. 1-2, pp. 155–160, 2001. View at Publisher • View at Google Scholar • View at Scopus
22. Tan R., She Z., M. Wang, Z. Fang, Y. Liu, and Q. Feng, “Thermo-sensitive alginate-based injectable hydrogel for tissue engineering,” Carbohydrate Polymers, vol. 87, no. 2, pp. 1515–1521, 2012. View at Publisher • View at Google Scholar • View at Scopus .
23. Liu G., X. Li, S. Xiong et al., “Fluorine-containing thermo-sensitive core/shell microgel particles: preparation, characterization, and their applications in controlled drug release,” Journal of Fluorine Chemistry, vol. 135, pp. 75–82, 2012. View at Publisher • View at Google Scholar • View at Scopus
24. Chen C. J., Q. Jin, G. Y. Liu, D. D. Li, J. L. Wang, and J. Ji, “Reversibly light-responsive micelles constructed via a simple modification of hyperbranched polymers with chromophores,” Polymer, vol. 53, no. 17, pp. 3695–3703, 2012. View at Publisher • View at Google Scholar
25. Husseini G. A., Velluto D., L. Kherbeck, W. G. Pitt, J. A. Hubbell, and D. A. Christensen, “Investigating the acoustic release of doxorubicin from targeted micelles,” Colloids and Surfaces B, vol. 101, pp. 153–155, 2013. View at Publisher • View at Google Scholar
26. Yin T., Wang P., Li J. et al., “Ultrasound-sensitive siRNA-loaded nanobubbles formed by hetero-assembly of polymeric micelles and liposomes and their therapeutic effect in gliomas,” Biomaterials, vol. 34, no. 18, pp. 4532–4543, 2013. View at Publisher • View at Google Scholar .
27. Tang B. C., Dawson M., Lai S. K. et al., “Biodegradable polymer nanoparticles that rapidly penetrate the human mucus barrier,” Proceedings of the National Academy of Sciences of the United States of America, vol. 106, no. 46, pp. 19268–19273, 2009. View at Publisher • View at Google Scholar • View at Scopus .
28. Cone R. A., “Barrier properties of mucus,” Advanced Drug Delivery Reviews, vol. 61, no. 2, pp. 75–85, 2009. View at Publisher • View at Google Scholar • View at Scopus
29. Rahmat D., Muller C., Barthelmes J., Shahnaz G., R. Martien, and Schnurch A. B., “Thiolated hydroxyethyl cellulose: design and in vitro evaluation of mucoadhesive and permeation enhancing nanoparticles,” European Journal of Pharmaceutics and Biopharmaceutics, vol. 83, no. 2, pp. 149–155, 2013. View at Publisher • View at Google Scholar
30. Srivalli K. M. R., Lakshmi P. K., and Balasubramaniam J., “Design of a novel bilayered gastric mucoadhesive system for localized and unidirectional release of lamotrigine,” Saudi Pharmaceutical Journal, vol. 21, no. 1, pp. 45–52, 2013. View at Publisher • View at Google Scholar • View at Scopus
31. Latere Dwan’Isa JP, Rouxhet L, Preat V, Brewster ME, Arien A. Prediction of drug solubility in amphiphilic di-block copolymer micelles: the role of polymer-drug compatibility. Pharmazie. 2007;62(7):499–504.
32. Coffman R, Kildsig D. Hydrotropic solubilization—mechanistic studies. Pharm Res. 1996; 13(10):1460–3.
33. Bauduin P, Renoncourt A, Kopf A, Touraud D, Kunz W. Unified concept of solubilization in water by hydrotropes and cosolvents. Langmuir. 2005; 21(15):6769–75.
34. Kim JY, Kim S, Papp M, Park K, Pinal R. Hydrotropic solubilization of poorly water-soluble drugs. J Pharm Sci. 2010; 99(9):3953–65.
35. Cui Y. Parallel stacking of caffeine with riboflavin in aqueous solutions: the potential mechanism for hydrotropic solubilization of riboflavin. Int J Pharm. 2010; 397(1–2):36–43.
36. Ooya T, Lee S, Huh K, Park K. Hydrotropic nanocarriers for poorly soluble drugs. In: Mozafari MR, editor. Nanocarrier technologies. Netherlands: Springer; 2006. p. 51–73.
37. Yu L, Bridgers A, Polli J, Vickers A, Long S, Roy A, et al. Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability. Pharm Res. 1999; 16(12):1812–7.
38. Muthu MS, Kulkarni SA, Xiong J, Feng SS. Vitamin E TPGS coated liposomes enhanced cellular uptake and cytotoxicity of docetaxel in brain cancer cells. Int J Pharm. 2011; 421(2):332–40.
39. Zhang Z, Feng SS. Nanoparticles of poly(lactide)/vitamin E TPGS copolymer for cancer chemotherapy: synthesis, formulation, characterization and in vitro drug release. Biomaterials. 2006; 27(2):262–70.
40. Liu Y, Huang L, Liu F. Paclitaxel nanocrystals for overcoming multidrug resistance in cancer. Mol Pharm. 2010;7(3):863–9.
41. Cheng X, Developing organic and inorganic nanomedicine for cancer therapy, Journal of Drug Delivery and Therapeutics. 2017; 7(2):1-4
42. Varma MV, Panchagnula R. Enhanced oral paclitaxel absorption with vitamin E-TPGS: effect on solubility and permeability in vitro, in situ and in vivo. Eur J Pharm Sci. 2005; 25(4–5):445– 53.
43. Cao N, Feng SS. Doxorubicin conjugated to D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS): conjugation chemistry, characterization, in vitro and in vivo evaluation. Biomaterials. 2008; 29(28):3856–65.
44. Huang Y, Lu J, Gao X, Li J, Zhao W, Sun M, et al. PEGderivatized embelin as a dual functional carrier for the delivery of paclitaxel. Bioconjug Chem. 2012; 23(7):1443–51.
45. Lu J, Huang Y, Zhao W, Marquez RT, Meng X, Li J, et al. PEGderivatized embelin as a nanomicellar carrier for delivery of paclitaxel to breast and prostate cancers. Biomaterials. 2013; 34(5):1591–600.
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).