Mucoadhesive acrylated block copolymers micelles for the delivery of hydrophobic drugs
Abstract
Blockpolymer micelles having acrylated end groups were fabricated for the development of mucoadhesive drug loaded vehicle. The critical micelle concentration (CMC) of Pluronic(®) F127 modified with acrylate end groups (F127DA) was found to be similar to that of the unmodified Pluronic(®) F127 (F127). Small angle X-ray scattering verified existence of micelles with an inner core of 4.9±0.2 and 5.5±0.3 for F127 and F127DA respectively. Indomethacin, a hydrophobic drug, was incorporated into the micelles using the thin-film hydration method. In vitro drug release assay demonstrated that the micelles sustained the release of the drug in comparison with free drug in solution. Several methods were used for mucoadhesion evaluation. Viscosity profiling was performed by shear rate sweep experiment of hydrated commercial mucin, F127 or F127DA, and combination of both mucin and a copolymer. Elevated viscosity was achieved for acrylated micelles with mucin compared to mixtures of non-acrylated micelles with mucin. The mucoadhesivity of the acrylated micelles was further characterized using nuclear magnetic resonance (NMR); data affirmed the Michael type addition reaction occurred between acrylates on the micelles corona and thiols present in the mucin. SAXS scattering data further showed a modification in the scattering of F127DA micelles with the addition of pig gastric mucin. Cryo-transmission electron microscopy (cryo-TEM) and dynamic light scattering (DLS) data detected increase in the aggregates size while using acrylated micelles enhance mucoadhesion. Thus acrylated F127DA micelles were found to be mucoadhesive, and a suitable and preferred candidate for micellar drug delivery to mucosal surfaces.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
CTAB micelles at 0.15 M and 30°C without NaNO3 were spheroidal; addition of 0.02 M NaNO3 resulted in a sphere-to-rod transition with both spheroids and worm-like micelles; in the presence of 0.04 M NaNO3 only rod-like structures were present.
“Micelles of CTAB without NaNO 3 were spheroidal, as illustrated in Fig. 9A.On the contrary, addition of 0.02 M NaNO 3 resulted in a sphere-to-rod transition, and both spheroids and worm-like micelles were found (Fig. 9B).Finally, in the presence of 0.04 M NaNO 3. only rod-like structures are present (Fig. 9C).”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [184]
Cites
Micellar Nanocarriers: Pharmaceutical Perspectives
Torchilin, V. P. (2006) · Pharmaceutical Research · doi:10.1007/s11095-006-9132-0 · Cited by 1,910 · see citing works
Pedersen, J. S. (1997) · Advances in Colloid and Interface Science · doi:10.1016/s0001-8686(97)00312-6 · Cited by 1,653 · see citing works
Mucoadhesive drug delivery systems
Donnelly, R. F., Shaikh, R., Singh, T. R. R., Garland, M. J., & Woolfson, A. D. (2011) · Journal of Pharmacy And Bioallied Sciences · doi:10.4103/0975-7406.76478 · Cited by 743 · see citing works
Mucoadhesive drug delivery system: An overview
Boddupalli, B. M., Mohammed, Z. K., Nath, R., & Banji, D. (2010) · Journal of Advanced Pharmaceutical Technology amp Research · doi:10.4103/0110-5558.76436 · Cited by 542 · see citing works
Sosnik, A., das Neves, J., & Sarmento, B. F. C. C. (2014) · Progress in Polymer Science · doi:10.1016/j.progpolymsci.2014.07.010 · Cited by 489 · see citing works
Scattering Form Factor of Block Copolymer Micelles
Pedersen, J. S., & Gerstenberg, M. C. (1996) · Macromolecules · doi:10.1021/ma9512115 · Cited by 454 · see citing works
Comparison of the mucoadhesive properties of various polymers
Grabovac, V., Guggi, D., & Bernkop‐Schnürch, A. (2005) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2005.07.006 · Cited by 451 · see citing works
A Simple Rheological Method for the in Vitro Assessment of Mucin-Polymer Bioadhesive Bond Strength
Hassan, E. E., & Gallo, J. M. (1990) · Pharmaceutical Research · doi:10.1023/a:1015812615635 · Cited by 439 · see citing works
La, S. B., Okano, T., & Kataoka, K. (1996) · Journal of Pharmaceutical Sciences · doi:10.1021/js950204r · Cited by 380 · see citing works
Form factors of block copolymer micelles with spherical, ellipsoidal and cylindrical cores
Pedersen, J. S. (2000) · Journal of Applied Crystallography · doi:10.1107/s0021889899012248 · Cited by 355 · see citing works
Bansil, R., Stanley, E., & LaMont, J. T. (1995) · Annual Review of Physiology · doi:10.1146/annurev.ph.57.030195.003223 · Cited by 352 · see citing works
Halstenberg, S., Panitch, A., Rizzi, S. C., Hall, H., & Hubbell, J. A. (2002) · Biomacromolecules · doi:10.1021/bm015629o · Cited by 315 · see citing works
Structure and Rheology Studies of Poly(oxyethylene−oxypropylene−oxyethylene) Aqueous Solution
Prud’homme, R. K., Wu, G., & Schneider, D. K. (1996) · Langmuir · doi:10.1021/la951506b · Cited by 301 · see citing works
Nanoscale technology of mucoadhesive interactions
Peppas, N. A., & Huang, Y. (2004) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2004.03.001 · Cited by 265 · see citing works
Nokhodchi, A., Javadzadeh, Y., Siahi‐Shadbad, M., et al. (2005) · PubMed · Cited by 220 · see citing works
Structure of Chitosan Determines Its Interactions with Mucin
Menchicchi, B., Fuenzalida, J. P., Bobbili, K. B., Hensel, A., Swamy, M. J., & Goycoolea, F. M. (2014) · Biomacromolecules · doi:10.1021/bm5007954 · Cited by 186 · see citing works
Effect of anti-inflammatories on Pluronic® F127: micellar assembly, gelation and partitioning
Sharma, P. K., & Bhatia, S. R. (2004) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2004.03.029 · Cited by 186 · see citing works
Zhang, W., Shi, Y., Chen, Y., Yu, S., Hao, J., Luo, J., Sha, X., & Fang, X. (2010) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2010.04.017 · Cited by 180 · see citing works
Goldmints, I., Yu, G., Booth, C., et al. (1999) · Langmuir · doi:10.1021/la9807006 · Cited by 177 · see citing works
Comparative rheological investigation of crude gastric mucin and natural gastric mucus
Kočevar-Nared, J., Kristl, J., & Šmid-Korbar, J. (1997) · Biomaterials · doi:10.1016/s0142-9612(96)00180-9 · Cited by 177 · see citing works
Mucoadhesive nanomedicines: characterization and modulation of mucoadhesion at the nanoscale
das Neves, J., Bahia, M. F., Amiji, M. M., & Sarmento, B. F. C. C. (2011) · Expert Opinion on Drug Delivery · doi:10.1517/17425247.2011.586334 · Cited by 156 · see citing works
Polymeric micelles in mucosal drug delivery: challenges towards clinical translation
Sosnik, A., & Menaker Raskin, M. (2015) · Biotechnology Advances · doi:10.1016/j.biotechadv.2015.01.003 · Cited by 154 · see citing works
Agüeros, M., Zabaleta, V., Espuelas, S., et al. (2010) · Journal of Controlled Release · doi:10.1016/j.jconrel.2010.03.012 · Cited by 153 · see citing works
Lopes, J. R., & Loh, W. (1998) · Langmuir · doi:10.1021/la9709655 · Cited by 150 · see citing works
Thiomers: potential excipients for non-invasive peptide delivery systems
Bernkop‐Schnürch, A., Krauland, A. H., Leitner, V. M., & Palmberger, T. F. (2004) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2004.03.032 · Cited by 143 · see citing works
Biophysical Analysis of the Molecular Interactions between Polysaccharides and Mucin
Menchicchi, B., Fuenzalida, J. P., Hensel, A., Swamy, M. J., David, L., Rochas, C., & Goycoolea, F. M. (2015) · Biomacromolecules · doi:10.1021/bm501832y · Cited by 142 · see citing works
Fang, X., Chen, Sha, X., Jiang, Chen, Y., & Ren (2013) · International Journal of Nanomedicine · doi:10.2147/ijn.s38221 · Cited by 140 · see citing works
Bioadhesive properties and rheology of polyether-modified poly(acrylic acid) hydrogels
Bromberg, L. E., Temchenko, M., Alakhov, V. Y., & Hatton, T. A. (2004) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2004.05.030 · Cited by 120 · see citing works
Viscometric study of pectin–mucin interaction and its mucoadhesive bond strength
Thirawong, N., Kennedy, R. A., & Sriamornsak, P. (2007) · Carbohydrate Polymers · doi:10.1016/j.carbpol.2007.05.026 · Cited by 113 · see citing works
Aw, M. S., Gulati, K., & Lošić, D. (2011) · Journal of Biomaterials and Nanobiotechnology · doi:10.4236/jbnb.2011.225058 · Cited by 106 · see citing works
Mucoadhesive Drug Delivery Systems
Hombach, J., & Bernkop‐Schnürch, A. (2009) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-00477-3_9 · Cited by 102 · see citing works
Ivarsson, D., & Wahlgren, M. (2011) · Colloids and Surfaces B Biointerfaces · doi:10.1016/j.colsurfb.2011.12.020 · Cited by 101 · see citing works
Alginate–PEGAc: A new mucoadhesive polymer
Davidovich‐Pinhas, M., & Bianco‐Peled, H. (2010) · Acta Biomaterialia · doi:10.1016/j.actbio.2010.09.021 · Cited by 96 · see citing works
Self-citationEvaluating the mucoadhesive properties of drug delivery systems based on hydrated thiolated alginate
Davidovich‐Pinhas, M., Harari, O., & Bianco‐Peled, H. (2009) · Journal of Controlled Release · doi:10.1016/j.jconrel.2009.01.029 · Cited by 96 · see citing works
Self-citationSun, Y., Liu, S., Du, G., Gao, G., & Fu, J. (2015) · Chemical Communications · doi:10.1039/c4cc10094h · Cited by 92 · see citing works
Fefelova, N. A., Nurkeeva, Z. S., Mun, G. A., et al. (2007) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2007.02.019 · Cited by 89 · see citing works
Chayed, S., & Winnik, F. M. (2006) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2006.08.017 · Cited by 88 · see citing works
Lian, H., Zhang, T., Sun, J., Liu, X., Ren, G., Kou, L., Zhang, Y., Han, X., Ding, W., Ai, X., et al. (2013) · Molecular Pharmaceutics · doi:10.1021/mp400282r · Cited by 82 · see citing works
Lopedota, A. A., Trapani, A., Cutrignelli, A., Chiarantini, L., Pantucci, E., Curci, R., Manuali, E., & Trapani, G. (2009) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2009.02.013 · Cited by 80 · see citing works
Mucoadhesive Drug Delivery Systems
Muppalaneni, S., Mastropietro, D. J., & Omidian, H. (2013) · doi:10.1002/9781118747896.ch10 · Cited by 73 · see citing works
Ding, H. Y., Yong, K., Law, W., Roy, I., Hu, R., Wu, F. P., Zhao, W., Huang, K., Erogbogbo, F., Bergey, E. J., et al. (2011) · Nanoscale · doi:10.1039/c1nr00001b · Cited by 67 · see citing works
Štorha, A., Mun, E. A., & Khutoryanskiy, V. V. (2013) · RSC Advances · doi:10.1039/c3ra42093k · Cited by 57 · see citing works
Thiol-Functionalized Polymeric Micelles: From Molecular Recognition to Improved Mucoadhesion
Dufresne, M.-H., Gauthier, M. A., & Leroux, J. (2005) · Bioconjugate Chemistry · doi:10.1021/bc050007b · Cited by 56 · see citing works
Bonferoni, M. C., Sandri, G., Ferrari, F., Rossi, S., Larghi, V., Zambito, Y., & Caramella, C. M. (2010) · Journal of Drug Delivery Science and Technology · doi:10.1016/s1773-2247(10)50073-x · Cited by 53 · see citing works
Dithiol-PEG-PDLLA Micelles: Preparation and Evaluation as Potential Topical Ocular Delivery Vehicle
Yang, J. Y., Yan, J., Zhou, Z., & Amsden, B. G. (2014) · Biomacromolecules · doi:10.1021/bm4018879 · Cited by 52 · see citing works
Novel mucoadhesive system based on sulfhydryl-acrylate interactions
Davidovich‐Pinhas, M., & Bianco‐Peled, H. (2010) · Journal of Materials Science Materials in Medicine · doi:10.1007/s10856-010-4069-6 · Cited by 50 · see citing works
Self-citationInteractions between Mucin and Surfactants at Solid−Liquid Interfaces
Dédinaité, A., & Bastardo, L. A. (2002) · Langmuir · doi:10.1021/la0259813 · Cited by 48 · see citing works
Mantle, M., Stewart, G. R., Zayas, G., et al. (1990) · PubMed · Cited by 35 · see citing works
Physical and structural characteristics of acrylated poly(ethylene glycol)–alginate conjugates
Davidovich‐Pinhas, M., & Bianco‐Peled, H. (2011) · Acta Biomaterialia · doi:10.1016/j.actbio.2011.04.001 · Cited by 34 · see citing works
Self-citationMicroporous membrane drug delivery system for indomethacin
Elchidana, P. A., & Deshpande, S. G. (1999) · Journal of Controlled Release · doi:10.1016/s0168-3659(98)00162-x · Cited by 27 · see citing works
Lafitte, G., Thuresson, K., & Söderman, O. (2005) · Langmuir · doi:10.1021/la0472807 · Cited by 23 · see citing works
Nanostructure Formation in the Lecithin/Isooctane/Water System
Koifman, N., Schnabel‐Lubovsky, M., & Talmon, Y. (2013) · The Journal of Physical Chemistry B · doi:10.1021/jp405490q · Cited by 21 · see citing works
Solubilization of Ibuprofen in Pluronic Block Copolymer F127 Micelles
Dong-Hua, W., Zheng, O., Yan, Z., et al. (2010) · Acta Physico-Chimica Sinica · doi:10.3866/pku.whxb20101207 · Cited by 18 · see citing works
Delivery of Methotrexate Executed by Engineered Polymeric Micelles Intended to Improve Chemotherapy
Kumar, B., Meher, J. G., Gupta, A., et al. (2014) · Journal of Biomaterials and Tissue Engineering · doi:10.1166/jbt.2014.1219 · Cited by 8 · see citing works
Pohmann, R. (2011) · Methods in molecular biology · doi:10.1007/978-1-61779-219-9_1 · Cited by 6 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Ghezzi, M., Pescina, S., Padula, C., Santi, P., Del Favero, E., Cantù, L., & Nicoli, S. (2021) · Journal of Controlled Release · doi:10.1016/j.jconrel.2021.02.031 · Cited by 1,135 · see citing works
Polymeric mixed micelles as nanomedicines: Achievements and perspectives
Cagel, M., Tesan, F. C., Bernabeu, E., Salgueiro, M. J., Zubillaga, M. B., Moretton, M. A., & Chiappetta, D. A. (2017) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2016.12.019 · Cited by 417 · see citing works
- Authors
- Eshel-Green, T., & Bianco-Peled, H.
- Affiliations
- Technion – Israel Institute of Technology (IL)
- Venue
- Colloids and Surfaces B Biointerfaces
- Publisher
- Elsevier BV
- Published
- 2016-03
- Volume
- 139
- Pages
- 42-51
- ISSN
- 0927-7765 (ISSN-L)
- OpenAlex
- W2238561937
- Cited by
- 57
- References
- 55
- Citations by year
- 2026: 1 · 2025: 7 · 2024: 6 · 2023: 7 · 2022: 4 · 2021: 4 · 2020: 5 · 2019: 6 · 2018: 5 · 2017: 8 · 2016: 4
- FWCI
- 3.15
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Colloids and Surfaces B Biointerfaces (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Chemistry › Physical and Theoretical Chemistry › Surfactants and Colloidal Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- Pluronic F127, block copolymer micelles, mucoadhesion, hydrophobic drug delivery, indomethacin, mucin, gastric mucin, sustained drug release, critical micelle concentration, Michael addition, mucosal drug delivery
- MeSH terms
- Acrylates, Animals, Drug Carriers, Drug Compounding, Gastric Mucins, Indomethacin, Kinetics, Micelles, Swine, Viscosity, Poloxamer, Hydrophobic and Hydrophilic Interactions, Drug Liberation
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
