Beck, Ruy Carlos Ruver

Fontana, Márcia Camponogara

Guterres, Silvia Stanisçuaski

Pohlmann, Adriana Raffin

English

Lume 5.8

caderno d•farmácla ISSN 0102-6593 Órgão Oficial da Faculdade de Farmácia da Universidade Federal do Rio Grande do Sul volume 26, Suplemento, 201 O 220 TECNOLOGIA FARMACÊUTICA E BIOFARMÁCIA Pharmaceutical technology and biopharmacy DEVELOPMENT OF RALOXIFENE-LOADED INNOVATIVE NANOPARTICLES PREPARED BY NANO SPRAY DRYER® Fontana M.C.1'; Pohlmann A. R.2 ; Guterres S. 8. 1; Beck R.C.R. 1 1 Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, UFRGS. 2Departamento de Química Orgânica, Instituto de Química, UFRGS. *Doutoranda -Início: 2010/1 lntroduction: Raloxifene is a nonsteroidal benzothiophene derivativa, administered orally for the treatment and prevention of osteoporosis in postmenopausal women and also to reduce the risk of breast cancer in postmenopausal women with osteoporosis.1 This drug acts also in reducing the fracture risk and its effects on the uterus and on the cardiovascular system are still being studied2. Moreover, the applicability of raloxifene on the treatment and prevention of neurodegenerative diseases related to age, like Alzheimer's disease, have also been focus of some researches. 3 After oral administration, raloxifene is rapidly absorbed (60 %) from the gastrointestinal tract and its absoluta bioavailability is just 2 %.4 1n this context, the nanosystems has advantages in providing a control drug release, increasing its bioavailability and facilitating their transport across biological barriers.5 Different preparation methods of nanoparticles are described in the literatura. However, a new possibility of preparation is being introduced through a new equipment called Nano Spray Dryer B-90 (Büchi, Switzerland). lt uses a vibrating mesh to generate fine aerosol droplets, a laminar drying ai r flow in the spray chamber and an electrostatic particle collector. The combination of innovative atomization principie and resourceful product separation technology providas the opportunity to utilize this spray drying technique for a variety of new applications.6 Objective: In this study we are proposing the development of biodegradable polymeric nanoparticles containing raloxifene (raloxifene hydrochloride) by the new technique of nano spray drying. Considering the low bioavailability of raloxifene, the potential of polymeric nanostructured systems as drug delivery systems and the activity of raloxifene on the treatment and prevention of Alzheimer's disease, this study has as main purpose to study the increase in effectiveness of this drug by the development of these innovative polymeric nanoparticles. Materiais and methods: Nanoparticles will be prepared by the nano spray drying technique (Nano Spray Dryer Büchi®- Advanced Model B-90), using different polymers and organic solvents. The quali-quantitative formulation will be optimized as well as the operational parameters. The physicochemical characteristics of the formulations will be monitored by drug content, encapsulation efficiency, mean size, polydispersity index, pH, zeta potential, and morphological analysis. In vitro drug release studies will be conducted by the dialysis bag method. The neuroprotective effect of raloxifene-loaded nanoparticles on the lesions induced by A~ peptide in hippocampal cultura model will be evaluated.7 In addition, the effect of raloxifene-loaded nanoparticles on depression and cognitiva impairment after its intraperitoneal administration in ovarectomized rats will be analyzed through the forced swim test and the test of Morris water maze.8 References: 1. K.C. Morello et a/., Clin. Pharmacokinet. 42, 361 (2003). 2. P.D. Delmas et a/., J. Med. 337, 23 (1997). 3. K. Yaffe et ai., Am. J. Psych. 162, 683 (2005). 4. M.J. Kayath, Arq. Bras. Endocrinol. Metab. 43, 433 (1999). 5. M. Rawat et a/., Biol. Pharmaceut. Buli. 29, 1790 (2006) 6. K. Schmid et ai., Respirat. Drug De/. Eur. 323 (2009). 7. L. Stoppini et a/., J. Neurosci. Meth. 37, 173 (1991 ). 8. M.J. Karahancer et a/., Fert. Steri/. 89, 240 (2008). Acknowldgements: The authors thank the financiai support from Instituto Nacional de Ciência e Tecnologia para Inovação Farmacêutica/INCT_IF, CNPq and Rede Nanocosméticos/CNPq. M.C.F. thanks CAPES/Brazil for her scholarship. 

Development of raloxifene-loaded innovative nanoparticles prepared by nano spray dryer

https://lume.ufrgs.br/bitstream/10183/267798/1/000770533.pdf

Development of raloxifene-loaded innovative nanoparticles prepared by nano spray dryer

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