Mucoadhesive liposomes offer a potential for improved residence time of liposomal systems targeting contact with mucosal tissues, such as in buccal, oral, colon, and vaginal drug delivery. Most of the currently available methods rely on the coating of preformed liposomes by various mucoadhesive polymers. The aim of this study was to develop novel mucoadhesive system by the one-pot preparation method. The pectin- and chitosan-containing liposomes, namely pectosomes and chitosomes, were prepared by the modified solvent injection method. In order to optimize this novel delivery system, we used pectins and chitosans of both high and low degree of esterification/deacetylation (DE/DD), respectively. Sonication was applied to reduce the original vesicle size. All vesicles were characterized for their size, zeta potential, metronidazole entrapment, and stability. Both pectosomes and chitosomes were found to entrap more metronidazole than conventional plain liposomes. Preliminary data indicate that the polymer is present on the liposomal surface, embedded within inner liposomal bilayers, and entrapped inside the aqueous compartment. The next step in the evaluation of this system is the testing of its mucoadhesiveness.
Vani？, ？.; ？kalko-Basnet, N. Nanopharmaceuticals for improved topical vaginal delivery: Can they deliver? Eur. J. Pharm. Sci. 2013, 50, 29–41, doi:10.1016/j.ejps.2013.04.035.
[3]
Das Neves, J.; Amiji, M.; Sarmento, B. Mucoadhesive nanosystems for vaginal microbicide development: Friend or foe? Wiley Interdiscip. Rev. Nanomed. Nanobiotechnol. 2011, 3, 389–399, doi:10.1002/wnan.144.
[4]
Valenta, C. The use of mucoadhesive polymers in vaginal delivery. Adv. Drug Deliver. Rev. 2005, 57, 1692–1712, doi:10.1016/j.addr.2005.07.004.
[5]
Bernkop-Schnürch, A.; Dünnhaupt, S. Chitosan-based drug delivery systems. Eur. J. Pharm. Biopharm. 2012, 81, 463–469, doi:10.1016/j.ejpb.2012.04.007.
[6]
Hagesaether, E.; Sande, S.A. In vitro measurements of mucoadhesive properties of six types of pectin. Drug Dev. Ind. Pharm. 2007, 33, 417–425, doi:10.1080/03639040600920630.
[7]
Sriamornsak, P. Application of pectin in oral drug delivery. Expert Opin. Drug Deliv. 2011, 8, 1009–1023, doi:10.1517/17425247.2011.584867.
[8]
Klemetsrud, T.; Jonassen, H.; Hiorth, M.; Kj？niksen, A.-L.; Smistad, G. Studies on pectin-coated liposomes and their interaction with mucin. Colloids Surf. B Biointerfaces 2013, 103, 158–165, doi:10.1016/j.colsurfb.2012.10.012.
[9]
Ogończyk, D.; Siek, M.; Garstecki, P. Microfluidic formulation of pectin microbeads for encapsulation and controlled release of nanoparticles. Biomicrofluidics 2011, 5, 013405:1–013405:12.
[10]
Sharma, R.; Ahujaa, M.; Kaur, H. Thiolated pectin nanoparticles: Preparation, characterization and ex vivo corneal permeation study. Carbohydr. Polym. 2012, 87, 1606–1610, doi:10.1016/j.carbpol.2011.09.065.
[11]
Burapapadha, K.; Kumpugdee-Vollrathc, M.; Chantasartd, D.; Sriamornsak, P. Fabrication of pectin-based nanoemulsions loaded with itraconazole for pharmaceutical application. Carbohydr. Polym. 2010, 82, 384–393, doi:10.1016/j.carbpol.2010.04.071.
[12]
Nguyen, S.; Alund, S.J.; Hiorth, M.; Kj？niksen, A.-L.; Smistad, G. Studies on pectin coating of liposomes for drug delivery. Colloids Surf. B Biointerfaces 2011, 88, 664–673, doi:10.1016/j.colsurfb.2011.07.058.
[13]
Karn, P.R.; Vani？, ？.; Pepi？, I.; ？kalko-Basnet, N. Mucoadhesive liposomal delivery systems: The choice of coating material. Drug Dev. Ind. Pharm. 2011, 37, 482–488, doi:10.3109/03639045.2010.523425.
[14]
Takeuchi, H.; Yamamoto, H.; Niwa, T.; Hino, T.; Kawashima, Y. Mucoadhesion of polymer-coated liposomes to rat intestine in vitro. Chem. Pharm. Bull. 1994, 42, 1954–1956, doi:10.1248/cpb.42.1954.
[15]
Manconi, M.; Mura, S.; Manca, M.L.; Fadda, A.M.; Dolz, M.; Hernandez, M.J.; Casanovas, A.; Díez-Sales, O. Chitosomes as drug delivery systems for C-phycocyanin: Preparation and characterization. Int. J. Pharm. 2010, 392, 92–100, doi:10.1016/j.ijpharm.2010.03.038.
[16]
Vani？, ？.; Hafner, A.; Bego, M.; ？kalko-Basnet, N. The characterization of various deformable liposomes with metronidazole. Drug Dev. Ind. Pharm. 2013, 39, 481–488, doi:10.3109/03639045.2012.670247.
[17]
Gentine, P.; Bubel, A.; Crucifix, C.; Bourel-Bonnet, L.; Frisch, B. Manufacture of liposomes by isopropanol injection: Characterisation of the method. J. Liposome Res. 2012, 22, 18–30, doi:10.3109/08982104.2011.584318.
[18]
Bartlett, G.R. Phosphorus assay in column chromatography. J. Biol. Chem. 1959, 234, 466–468.
[19]
？kalko, N.; ？ajkovac, M.; Jal？enjak, I. Liposomes with metronidazole for topical use: The choice of preparation method and vehicle. J. Liposome Res. 1998, 8, 283–293, doi:10.3109/08982109809035532.
[20]
Di Cagno, M.; Styskala, J.; Hlavá？, J.; Brandl, M.; Bauer-Brandl, A.; ？kalko-Basnet, N. Liposomal solubilization of new 3-hydroxy-quinolinone derivatives with promising anticancer activity: A screening method to identify maximum incorporation capacity. J. Liposome Res. 2011, 21, 272–278, doi:10.3109/08982104.2010.550265.
[21]
Basnet, P.; Hussain, H.; Tho, I.; ？kalko-Basnet, N. Liposomal delivery system enhances anti-inflammatory properties of curcumin. J. Pharm. Sci. 2012, 101, 598–609, doi:10.1002/jps.22785.
