Molecular implications in the nanoencapsulation of the anti-tuberculosis drug rifampicin within flower-like polymeric micelles
Abstract
Tuberculosis (TB) is the second most deadly infectious disease behind the Human Immunodeficiency Virus (HIV). An effective pharmacotherapy has been available for more than 5 decades. However, the length of the treatment and the pill burden result in low patient compliance and adherence to the regimens. Nanotechnologies can overcome these basic technological drawbacks. The present work explored the molecular implications governing the encapsulation and water solubilization of RIF within flower-like micelles of poly(epsilon-caprolactone)-b-poly(ethylene glycol)-poly(epsilon-caprolactone) (PCL-PEG-PCL) block copolymers. Ten derivatives of different molecular weight and hydrophobic/hydrophilic caprolactone/ethylene oxide ratio (CL/EO) were synthesized by a fast and high-yield Microwave-Assisted Polymer Synthesis (MAPS) technique; CL/EO values are determined by taking the ratios of the number of repeating units in the PCL and the PEG segments. The aggregation behavior of the copolymers was thoroughly investigated by means of surface tension (critical micellar concentration), dynamic light scattering (size, size distribution and zeta potential) and transmission electron microscopy (morphology). In general, the greater the central PEG segment, the larger the micelles formed. The physical stability was intimately associated with the molecular weight and the composition. Then, the encapsulation of RIF in the different copolymer families was evaluated, and the physical stability of the…
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For stimuli-responsive micelles, DLS can give preliminary information regarding nanocarriers behavior when undergoing pH or other environmental conditions variations.
“Additionally, in the case of stimuli-responsive micelles, this technique can give preliminary information regarding nanocarriers behavior when undergoing pH or other environmental conditions variations [135,136].”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [136]
This evidence, combined with TEM and FRET data, supports the use of these stimuli-responsive micelles for site-specific drug delivery to tissues characterized by high levels of oxidative stress.
“This evidence, combined with TEM and FRET data, supports the use of these stimuliresponsive micelles for site-specific drug delivery to tissues characterized by high levels of oxidative stress [136].”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [136]
Emission spectra obtained after 10-fold dilution either with PBS or with dimethylformamide (DMF) confirmed the effectiveness of the technique in demonstrating micelle integrity (PBS) or disassembly (DMF).
“The emission spectra obtained after 10-fold dilution either with PBS or with dimethylformamide (DMF) confirmed the effectiveness of the technique in demonstrating micelle integrity (PBS) or disassembly (DMF) (Fig. 10C).”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [136]
Gupta et al. evaluated poly(PS74-b-DMA310) micelles assembly using DiO and DiI as FRET donor and acceptor.
“Gupta et al. [136] evaluated propylene sulfide (PS) and N,Ndimethylacrylamide (DMA) (poly(PS 74 -b-DMA 310 ) micelles assembly using as FRET dyes DiO and DiI, working respectively as donor and acceptor.”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [136]
Cites
Controlled Microwave Heating in Modern Organic Synthesis
Kappe, C. O. (2004) · Angewandte Chemie International Edition · doi:10.1002/anie.200400655 · Cited by 3,628 · see citing works
Analytical profiles of drug substances
(1975) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600640947 · Cited by 1,498 · see citing works
Block copolymer micelles: preparation, characterization and application in drug delivery
Gaucher, G., Dufresne, M.-H., Sant, V. P., Kang, N., Maysinger, D., & Leroux, J.-C. (2005) · Journal of Controlled Release · doi:10.1016/j.jconrel.2005.09.034 · Cited by 1,498 · see citing works
<i>Mycobacterium tuberculosis</i>Pathogenesis and Molecular Determinants of Virulence
Smith, I. (2003) · Clinical Microbiology Reviews · doi:10.1128/cmr.16.3.463-496.2003 · Cited by 1,154 · see citing works
Frieden, T. R., Sterling, T. R., Munsiff, S. S., Watt, C. J., & Dye, C. (2003) · The Lancet · doi:10.1016/s0140-6736(03)14333-4 · Cited by 718 · see citing works
Global epidemiology of tuberculosis
Dye, C. (2006) · The Lancet · doi:10.1016/s0140-6736(06)68384-0 · Cited by 717 · see citing works
Chiappetta, D. A., & Sosnik, A. (2007) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2007.03.022 · Cited by 570 · see citing works
Self-citationKabanov, A. V., Nazarova, I. R., Astafieva, I. V., Batrakova, E. V., Alakhov, V. Y., Yaroslavov, A. A., & Kabanov, V. A. (1995) · Macromolecules · doi:10.1021/ma00111a026 · Cited by 459 · see citing works
Annulling a dangerous liaison: vaccination strategies against AIDS and tuberculosis
Kaufmann, S. H. E., & McMichael, A. J. (2005) · Nature Medicine · doi:10.1038/nm1221 · Cited by 272 · see citing works
New old challenges in tuberculosis: Potentially effective nanotechnologies in drug delivery
Sosnik, A., Carcaboso, A. M., Glisoni, R. J., Moretton, M. A., & Chiappetta, D. A. (2009) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2009.11.023 · Cited by 264 · see citing works
Self-citationLetchford, K., Liggins, R., & Burt, H. (2008) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21037 · Cited by 254 · see citing works
Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers
Kumar, P. V., Asthana, A., Dutta, T., et al. (2006) · Journal of drug targeting · doi:10.1080/10611860600825159 · Cited by 216 · see citing works
Liu, J., Zeng, F., & Allen, C. (2007) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2006.11.010 · Cited by 183 · see citing works
Synthesis and characterization of PCL/PEG/PCL triblock copolymers by using calcium catalyst
Piao, L., Dai, Z., Deng, M., Chen, X., & Jing, X. (2003) · Polymer · doi:10.1016/s0032-3861(03)00087-9 · Cited by 178 · see citing works
Chiappetta, D. A., Höcht, C., Taira, C. A., & Sosnik, A. (2009) · Nanomedicine · doi:10.2217/nnm.09.90 · Cited by 174 · see citing works
Self-citationSelf-Associative Behavior and Drug-Solubilizing Ability of Poloxamine (Tetronic) Block Copolymers
González-López, J., Alvarez‐Lorenzo, C., Taboada, P., Sosnik, A., Sández-Macho, I., & Concheiro, Á. (2008) · Langmuir · doi:10.1021/la8016563 · Cited by 142 · see citing works
Self-citationNew anti-tuberculosis drugs in clinical trials with novel mechanisms of action
Rivers, E. C., & Mancera, R. L. (2008) · Drug Discovery Today · doi:10.1016/j.drudis.2008.09.004 · Cited by 140 · see citing works
Liposomes for drug delivery to the lungs by nebulization
Zaru, M., Mourtas, S., Klepetsanis, P. G., Fadda, A. M., & Antimisiaris, S. G. (2007) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2007.04.005 · Cited by 131 · see citing works
Shishoo, C. J., Shah, S. A., Rathod, I. S., et al. (2001) · International Journal of Pharmaceutics · doi:10.1016/s0378-5173(01)00831-6 · Cited by 127 · see citing works
Stability and release performance of a series of pegylated copolymeric micelles
Lin, W.-J., Juang, L.-W., & Lin, C.-C. (2003) · Pharmaceutical Research · doi:10.1023/a:1023215320026 · Cited by 125 · see citing works
Forrest, M. L., Yáñez, J. A., Remsberg, C. M., Ohgami, Y., Kwon, G. S., & Davies, N. M. (2007) · Pharmaceutical Research · doi:10.1007/s11095-007-9451-9 · Cited by 114 · see citing works
Schwach, G., & Vert, M. (1999) · International Journal of Biological Macromolecules · doi:10.1016/s0141-8130(99)00043-4 · Cited by 109 · see citing works
Treatment of tuberculosis: present status and future prospects.
Onyebujoh, P., Zumla, A. I., Ribeiro, I., et al. (2005) · PubMed · Cited by 97 · see citing works
Letchford, K., Liggins, R., Wasan, K. M., & Burt, H. M. (2008) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2008.08.003 · Cited by 89 · see citing works
Mariappan, T. T., & Singh, S. (2003) · PubMed · Cited by 84 · see citing works
Stability of rifampicin in dissolution medium in presence of isoniazid
Shishoo, C. J., Shah, S. A., Rathod, I. S., et al. (1999) · International Journal of Pharmaceutics · doi:10.1016/s0378-5173(99)00286-0 · Cited by 82 · see citing works
Biowaiver monographs for immediate release solid oral dosage forms: Rifampicin
Becker, C., Dressman, J., Junginger, H. E., et al. (2009) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21624 · Cited by 78 · see citing works
Singh, S., Mariappan, T. T., Sharda, N., et al. (2000) · Pharmacy and Pharmacology Communications · doi:10.1211/146080800128736277 · Cited by 78 · see citing works
Yang, Y., Hua, C., & Dong, C. (2009) · Biomacromolecules · doi:10.1021/bm900497z · Cited by 77 · see citing works
Triclosan-loaded poloxamine micelles for enhanced topical antibacterial activity against biofilm
Chiappetta, D. A., Degrossi, J., Teves, S., D’Aquino, M., Bregni, C., & Sosnik, A. (2008) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2007.11.021 · Cited by 65 · see citing works
Self-citationEffect of Molecular Mass on the Melting Temperature, Enthalpy and Entropy of Hydroxy-Terminated PEO
Sánchez-Soto, P. J., Gines, J. M., Arias, M., et al. (2002) · Journal of Thermal Analysis and Calorimetry · doi:10.1023/a:1013758518721 · Cited by 59 · see citing works
Polymeric Nanocarriers: New Endeavors for the Optimization of the Technological Aspects of Drugs
Sosnik, A., Carcaboso, A. M., & Chiappetta, D. A. (2008) · Recent Patents on Biomedical Engineering · doi:10.2174/1874764710801010043 · Cited by 55 · see citing works
Self-citationPoly(ethylene glycol)-poly(epsilon-caprolactone) block oligomers as injectable materials
Sosnik, A., & Cohn, D. (2003) · Polymer · doi:10.1016/j.polymer.2003.09.012 · Cited by 45 · see citing works
Self-citationZhao, Y., Liang, H., Wang, S., et al. (2001) · The Journal of Physical Chemistry B · doi:10.1021/jp003001m · Cited by 44 · see citing works
Changsan, N., Nilkaeo, A., Pungrassami, P., & Srichana, T. (2009) · Journal of drug targeting · doi:10.3109/10611860903079462 · Cited by 42 · see citing works
Dong, J., Armstrong, J. K., Chowdhry, B. Z., et al. (2004) · Thermochimica Acta · doi:10.1016/j.tca.2003.08.030 · Cited by 39 · see citing works
WHO declares tuberculosis a global emergency
World Health Organization (1993) · Sozial- und Präventivmedizin · doi:10.1007/bf01624546 · Cited by 39 · see citing works
Solubilisation of polyaromatic hydrocarbons in aqueous solutions of poloxamine T803
Dong, J., Chowdhry, B. Z., & Leharne, S. A. (2004) · Colloids and Surfaces A Physicochemical and Engineering Aspects · doi:10.1016/j.colsurfa.2004.07.006 · Cited by 38 · see citing works
Richter, A., Olbrich, C., Krause, M., Hoffmann, J., & Kissel, T. (2010) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2010.02.010 · Cited by 35 · see citing works
Agrawal, S., & Panchagnula, R. (2004) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2004.09.005 · Cited by 34 · see citing works
Rifamycins. LIX. Acetyl migration in rifampicin
Maggi, N., Vigevani, A., Gallo, G. G., et al. (1968) · Journal of Medicinal Chemistry · doi:10.1021/jm00311a004 · Cited by 26 · see citing works
Positioning of Rifampicin in the Biopharmaceutics Classification System (BCS)
Mariappan, T. T., & Singh, S. (2006) · Clinical Research and Regulatory Affairs · doi:10.1080/10601330500533990 · Cited by 25 · see citing works
Long Time Due: Reducing Tuberculosis Mortality in the 21st Century
Brewer, T. F., & Heymann, J. S. (2005) · Archives of Medical Research · doi:10.1016/j.arcmed.2005.06.002 · Cited by 21 · see citing works
Mehta, S. K., Bhasin, K. K., Mehta, N., et al. (2004) · Colloid & Polymer Science · doi:10.1007/s00396-004-1181-5 · Cited by 15 · see citing works
Hu, Y., Ding, Y., Li, Y., et al. (2006) · Journal of Nanoscience and Nanotechnology · doi:10.1166/jnn.2006.432 · Cited by 12 · see citing works
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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
Self-citationPolymeric 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
Self-citation
- Authors
- Moretton, M. A., Glisoni, R. J., Chiappetta, D. A., & Sosnik, A.
- Affiliations
- Consejo Nacional de Investigaciones Científicas y Técnicas (AR)
- Corresponding author
- Sosnik, Alejandro
- Venue
- Colloids and Surfaces B: Biointerfaces
- Publisher
- Elsevier BV
- Published
- 2010-09
- Volume
- 79
- Issue
- 2
- Pages
- 467-479
- ISSN
- 0927-7765 (ISSN-L)
- OpenAlex
- W1972528605
- Cited by
- 96
- References
- 45
- Citations by year
- 2026: 1 · 2025: 3 · 2024: 2 · 2023: 6 · 2022: 5 · 2021: 11 · 2020: 7 · 2019: 5 · 2018: 5 · 2017: 12 · 2016: 7 · 2015: 9 · 2014: 8 · 2013: 5 · 2012: 5
- FWCI
- 1.98
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Colloids and Surfaces B Biointerfaces (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Physical Sciences › Chemistry › Organic Chemistry › Surfactants and Colloidal Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- rifampicin, nanoencapsulation, flower-like micelles, polymeric micelles, polycaprolactone, polyethylene glycol, tuberculosis, drug solubilization, critical micelle concentration, micelle size, molecular weight effects, physical stability, drug delivery
- MeSH terms
- Antitubercular Agents, Calorimetry, Differential Scanning, Micelles, Particle Size, Polyesters, Polyethylene Glycols, Rifampin, Solubility, Temperature, Water, Nanotechnology, Nanostructures
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