DEVELOPMENT OF ORAL NIFEDIPINE-LOADED POLYMERIC NANOCAPSULES: PHYSICOCHEMICAL CHARACTERISATION, PHOTOSTABILITY STUDIES, IN VITRO AND IN VIVO EVALUATION

被引:9
作者
Tagliari, Monika Piazzon [1 ]
Granada, Andrea [1 ]
Segatto Silva, Marcos Antonio [1 ]
Stulzer, Hellen Karine [1 ]
Zanetti-Ramos, Betina Giehl [2 ]
Fernandes, Daniel [3 ]
Silva, Izabella Thais [4 ]
Oliveira Simoes, Claudia Maria [4 ]
Sordi, Regina [5 ]
Assreuy, Jamil [5 ]
Soldi, Valdir [6 ]
机构
[1] Univ Fed Santa Catarina, Ctr Ciencias Saude, Dept Ciencias Farmaceut, Florianopolis, SC, Brazil
[2] Nanovetores, Dept Pesquisa Desenvolvimento & Inovacao, Florianopolis, SC, Brazil
[3] Univ Estadual Ponta Grossa, Ctr Ciencias Saude, Dept Ciencias Farmaceut, Ponta Grossa, PR, Brazil
[4] Univ Fed Santa Catarina, Dept Ciencias Farmaceut, Florianopolis, SC, Brazil
[5] Univ Fed Santa Catarina, Dept Farmacol, Florianopolis, SC, Brazil
[6] Univ Fed Santa Catarina, Ctr Ciencias Fis & Matemat, Dept Quim, Florianopolis, SC, Brazil
来源
QUIMICA NOVA | 2015年 / 38卷 / 06期
关键词
nifedipine; nanocapsule; polymeric material; stability; CONTROLLED-RELEASE; NANOPARTICLES; DRUGS; MICROPARTICLES; MICROSPHERES; DISSOLUTION; STABILITY; SOLVENT; PHOTODECOMPOSITION; DISPERSION;
D O I
10.5935/0100-4042.20150076
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In this study, nifedipine (NFP)-loaded polymeric nanocapsules were prepared and characterised with a view to protect the drug from degradation. Nanocapsule suspensions were prepared using two different surfactants (pluronic F68 and polyvinyl alcohol). Physicochemical stability and in vivo antihypertensive effect were evaluated. The particle size, zeta potential and entrapment efficiency remained constant during a period of 28 days of exposure under light irradiation. A smaller particle size and a higher zeta potential were obtained for the nanocapsules prepared with Pluronic F68 as surfactant. The solid drug and the nanocapsules were submitted to light exposure for 28 days. After this period of time, the percentage of drug remaining in the PF68NFP and PVANFP nanocapsules was 28.1% and 21.3%, respectively. In contrast, the solid drug was completely degraded after 4 days, suggesting that the nanocapsule suspensions promoted significant protection of the drug against light exposure. In addition, in vivo studies were carried out, which demonstrated that the formulations with polyvinyl alcohol exhibited a very rapid onset of action after oral administration in rats and led to faster drug release. The nanoparticles developed can be considered as an alternative for improving NFP stability in liquid formulations.
引用
收藏
页码:781 / 786
页数:6
相关论文
共 45 条
[1]   Mechanisms of nanoparticle and bioparticle deposition - Kinetic aspects [J].
Adamczyk, Zbigniew ;
Nattich-Rak, Malgorzata ;
Sadowska, Marta ;
Michna, Aneta ;
Szczepaniak, Katarzyna .
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS, 2013, 439 :3-22
[2]  
Anton N, 2008, J CONTROL RELEASE, V128, P185, DOI 10.1016/j.jconrel.2008.02.007
[3]   Preparation of sodium alginate-methylcellulose blend microspheres for controlled release of nifedivine [J].
Babu, V. Ramesh ;
Sairam, Malladi ;
Hosamani, Kallappa M. ;
Aminabhavi, Tejraj M. .
CARBOHYDRATE POLYMERS, 2007, 69 (02) :241-250
[4]   Effect of inclusion complexation with cyclodextrins on photostability of nifedipine in solid state [J].
Bayomi, MA ;
Abanumay, KA ;
Al-Angary, AA .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 243 (1-2) :107-117
[5]   Atovaquone-loaded nanocapsules: influence of the nature of the polymer on their in vitro characteristics [J].
Cauchetier, E ;
Deniau, M ;
Fessi, H ;
Astier, A ;
Paul, M .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 250 (01) :273-281
[6]   Characterization and physical stability of fast-dissolving microparticles containing nifedipine [J].
Cilurzo, Francesco ;
Selmin, Francesca ;
Minghetti, Paola ;
Gennari, Chiara G. M. ;
Demartin, Francesco ;
Montanari, Luisa .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2008, 68 (03) :579-588
[7]   Factorial design as tool in chitosan nanoparticles development by ionic gelation technique [J].
de Pinho Neves, Andreia Lange ;
Milioli, Camila Cardoso ;
Mueller, Leidiani ;
Riella, Humberto Gracher ;
Kuhnen, Nivaldo Cabral ;
Stulzer, Hellen Karine .
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS, 2014, 445 :34-39
[8]   NANOCAPSULE FORMATION BY INTERFACIAL POLYMER DEPOSITION FOLLOWING SOLVENT DISPLACEMENT [J].
FESSI, H ;
PUISIEUX, F ;
DEVISSAGUET, JP ;
AMMOURY, N ;
BENITA, S .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 55 (01) :R1-R4
[9]   Effect of the non-ionic surfactant Poloxamer 188 on passive permeability of poorly soluble drugs across Caco-2 cell monolayers [J].
Fischer, Sarah Maud ;
Brandl, Martin ;
Fricker, Gert .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2011, 79 (02) :416-422
[10]   Nifedipine-Loaded Polymeric Nanocapsules: Validation of a Stability-Indicating HPLC Method to Evaluate the Drug Entrapment Efficiency and In Vitro Release Profiles [J].
Granada, Andrea ;
Tagliari, Monika Piazzon ;
Soldi, Valdir ;
Segatto Silva, Marcos Antonio ;
Zanetti-Ramos, Betina Ghiel ;
Fernandes, Daniel ;
Stulzer, Hellen Karine .
JOURNAL OF AOAC INTERNATIONAL, 2013, 96 (02) :276-281