The DOI matches its Crossref record; 4 of the 4 references it cites were found in a registry or an index.
Oral Delivery of Doxorubicin Using Novel Polyelectrolyte-Stabilized Liposomes (Layersomes)
Abstract
The present study explores the potential of polyelectrolyte-coated liposomes for improving the oral deliverability of doxorubicin (Dox). As a part of formulation strategy, stearyl amine was selected as a formulation component to provide positive charge to liposomes, which were subsequently coated with anionic poly(acrylic acid) (PAA) followed by coating of cationic polyallyl amine hydrochloride (PAH) in a layer by layer manner and led to the formation of a robust structure "layersomes". Optimization of various process variables were carried out, and optimized formulation was found to have particle size of 520.4 ± 15.0 nm, PDI of 0.312 ± 0.062, ζ potential of +30.4 ± 5.32 mV, and encapsulation efficiency of 63.4 ± 4.26%. Layersomes were not only stable in simulated gastrointestinal fluids but also presented sustained drug release (∼35%) as compared to both Dox-liposomes and PAA-Dox-liposomes (∼67%), the release pattern being Higuchi kinetics. The in vivo pharmacokinetics studies revealed about 5.94-fold increase in oral bioavailability of Dox as compared to free drug. In vivo antitumor efficacy in a DMBA-induced breast tumor model further exhibited significant reduction in the tumor growth as compared to control and IV-Dox, while results were comparable to IV-LipoDox. Layersomes also exhibited a marked reduction in cardiotoxicity in comparison with IV-doxorubicin and IV-LipoDox (marketed formulation), as evidenced by the reduced levels of malondialdehyde (MDA), lactate dehydrogenase (LDH), and creatine phosphokinase (CK-MB) and increased levels of glutathione (GSH) and superoxide dismutase (SOD). The reduced cardiotoxicity of layersomes was further confirmed by comparative histopathological examination of heart tissue after treatment with various formulations. The positive results of the study strengthen our expectation that the developed formulation strategy can be fruitfully exploited to improve the oral deliverability of poorly bioavailable drugs and can open new vistas for oral chemotherapy.
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Citations
Cites
Recent advances with liposomes as pharmaceutical carriers
Torchilin, V. P. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1632 · Cited by 5,282
Kalaria, D. R., Sharma, G., Beniwal, V., & Ravi Kumar, M. N. V. (2009) · Pharmaceutical Research · doi:10.1007/s11095-008-9763-4 · Cited by 246
Jain, A. K., Swarnakar, N. K., Godugu, C., Singh, R. P., & Jain, S. (2011) · Biomaterials · doi:10.1016/j.biomaterials.2010.09.037 · Cited by 232
Self-citationJain, A. K., Swarnakar, N. K., Das, M., Godugu, C., Singh, R. P., Rao, P. R., & Jain, S. (2011) · Molecular Pharmaceutics · doi:10.1021/mp200011f · Cited by 89
Self-citation
Cited by
Role of nanoparticle size, shape and surface chemistry in oral drug delivery
Banerjee, A., Qi, J., Gogoi, R., Wong, J., & Mitragotri, S. (2016) · Journal of Controlled Release · doi:10.1016/j.jconrel.2016.07.051 · Cited by 773
Adapting liposomes for oral drug delivery
He, H., Lu, Y., Qi, J., Zhu, Q., Chen, Z., & Wu, W. (2019) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2018.06.005 · Cited by 663
In vitro release kinetics model fitting of liposomes: An insight
Jain, A., & Jain, S. K. (2016) · Chemistry and Physics of Lipids · doi:10.1016/j.chemphyslip.2016.10.005 · Cited by 373
Self-citationLipid-based nanovesicles for nanomedicine
Grimaldi, N., Andrade, F., Segovia, N., Ferrer-Tasies, L., Sala, S., Veciana, J., & Ventosa, N. (2016) · Chemical Society Reviews · doi:10.1039/c6cs00409a · Cited by 309
Metadata
- Authors
- Jain, S., Patil, S. R., Swarnakar, N. K., & Agrawal, A. K.
- Venue
- Molecular Pharmaceutics
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-08-15
- Volume
- 9
- Issue
- 9
- Pages
- 2626-2635
- ISSN
- 1543-8384 (ISSN-L)
- 1543-8392
- OpenAlex
- W2034574681
- Cited by
- 158
- References
- 4
- FWCI
- 5.77
- Type
- journal article
- Language
- en
- Open access
- closed
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