Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery

Kwon, Suk Hyung; Kim, Sun Young; Ha, Kyung Won; Kang, Myung Joo; Huh, Jin Seo; Im, Tae Jong; Kim, Yong Min; Park, Young Mi; Kang, Kyung‐Hwa; Lee, Sang Kil; Chang, Jung Yun; Lee, Jaehwi; Choi, Young Wook

doi:10.1007/bf02980249

Cited by 96 publications

(45 citation statements)

References 17 publications

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“…Kelarutan genistein yang rendah dalam air, membatasi penggunaan secara klinis. Beberapa studi terdahulu untuk meningkatkan kelarutan dan laju disolusi genistein telah dilaporkan, diantaranya; pembuatan nanopartikel dan mikropartikel dengan polimer hidrofilik, pembuatan kompleks inklusi dan formulasi polimerik misel [10,11,12,13]. Tujuan dari penelitian ini, adalah memperbaiki laju disolusi genistein dengan teknik sistem dispersi padat menggunakan polimer hidrofilik PVP K-30 dan melakukan karakterisasi sistem dispersi padat yang terbentuk dengan analisa difraksi sinar-X, analisa termal DSC, analisa spektroskopi FT-IR dan analisa mikroskopik SEM.…”

Section: Pendahuluanunclassified

Peningkatan Laju Disolusi Dispersi Padat Amorf Genistein dengan PVP K-30

et al. 2017

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Amorphous solid dispersions of a poorly water-soluble drug genistein in PVP K-30 were prepared by solvent co-evaporation technique using organic solvent methanol. Solid dispersions system was prepared with several variations of the drug to polymer 2:1, 1:1 dan 1:2 w/w. Solid state properties of solid dispersion system were evaluated by powder X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry, and microscopic SEM. Dissolution rate profile was conducted in distilled water medium by using dissolution tester apparatus type II USP. Base on X-ray diffractometry analysis, differential scanning calorimetry and microscopic SEM, crystalline phase of genistein decreased in crystallinity index and formation of the amorphous state. Dissolution rate profile showed that genistein in amorphous solid dispersion had a faster dissolution rate in comparison to intact genistein. This study suggests that preparation of the solid dispersion of genistein in PVP K-30 is an effective approach to improve the dissolution rate of genistein. ABSTRAK:Sistem dispersi padat amorf senyawa obat yang sukar larut air genistein dalam PVP K-30 dibuat dengan metode penguapan pelarut menggunakan pelarut metanol. Sistem dispersi padat dibuat dengan variasi perbandingan obat : polimer 2:1, 1:1 dan 1:2 b/b. Sifat padatan serbuk sistem dispersi padat dievaluasi dengan metode analisa difraksi sinar-X, termal DSC, spektrokopik FT-IR dan mikroskopik SEM. Profil disolusi dilakukan dalam medium air suling dengan alat uji disolusi tipe II USP. Hasil analisa difraksi sinar-X, termal DSC dan mikroskopik SEM, fase kristalin genistein mengalami penurunan derajat kristalinitas dan pembentukan fase amorf. Profil laju disolusi menunjukkan bahwa sistem dispersi padat genistein memiliki laju disolusi yang lebih tinggi dibandingkan genistein murni. Studi ini membuktikan bahwa pembentukan sistem dispersi padat genistein dengan polimer PVP K-30 efektif memperbaiki laju disolusi genistein. Keywords 67 PENDAHULUANKelarutan dan laju disolusi senyawa obat yang rendah dalam air merupakan salah satu permasalahan besar dalam pengembangan dan manufaktur sediaan padat (tablet, kapsul) di industri farmasi. Lebih dari 80 % sediaan obat dipasaran adalah dalam bentuk tablet, dan 40 % dari senyawa obat tersebut memiliki kelarutan yang rendah dalam air, serta hampir 80 -90 % senyawa kandidat obat yang dalam tahap penelitian juga memiliki permasalahan kelarutan dan laju disolusi [1,2].Berdasarkan Biopharmaceutical classification system (BCS) senyawa obat diklasifikasi kedalam empat kategori, kelas I (kelarutan tinggi, permeabilitas tinggi), II (kelarutan rendah, permeabilitas tinggi), III (kelarutan tinggi, permeabilitas rendah dan kelas IV (kelarutan rendah, permeabilitas rendah) Senyawa obat yang masuk dalam kategori kelas II dan IV seringkali mengalami absorpsi yang rendah dalam cairan saluran pencernaan [3]. Berbagai strategi telah dilaporkan untuk memperbaiki laju disolusi senyawa obat kelas II dan IV ini, antara lain pembuata...

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Section: Pendahuluanunclassified

Peningkatan Laju Disolusi Dispersi Padat Amorf Genistein dengan PVP K-30

et al. 2017

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“…177 Pluronic F127 of average compositions EO 99 PO 67 EO 99 , showed increased oral delivery of genistein in rats compared to genistein powder. 178 The plasma AUC was three-fold higher at a dose of 4 mg/kg genistein in anesthetized rats (p > 0.5). The micelle particle size was on average 27 nm.…”

Section: Polymeric Micellesmentioning

confidence: 97%

Nanopreparations for Oral Administration

Hubbard

Brayden

Ghandehari

2014

Frontiers in Nanobiomedical Research

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Oral delivery has distinct advantages over parenteral administration. These include ease of administration and improved patient compliance. Physiological barriers to oral drug delivery include low pH environment of the stomach, high enzymatic activity of the small intestine, and poor permeability of large molecular weight and hydrophilic compounds across the gastrointestinal epithelial layer. These barriers reduce stability and absorption of drug molecules to the systemic circulation. In order to overcome these barriers, nanopreparations have been investigated for their potential in oral delivery. In this chapter, selected nanoscale formulations investigated for oral drug delivery are discussed.Handbook of Nanobiomedical Research Downloaded from www.worldscientific.com by UNIVERSITY OF QUEENSLAND on 02/03/15. For personal use only.

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“…However, there are other NPs such as solid lipid, polymeric micelles, and dendrimers that are reported in the literature, which are being explored for oral delivery. [38][39][40][41] In order to maximize the bioavailability of NPs following the oral route, we will examine the physiological barriers of the gastrointestinal (GI) tract. The primary function of the intestinal barriers is to allow nutrients to reach the systemic circulation while defending the body from the unwanted molecules.…”

Section: Oral Delivery Route For the Npsmentioning

confidence: 99%

Biological Requirement and Safety Assessment of Nanomedicines

Zolnik¹,

Bancos²,

Kim³

et al. 2014

Frontiers in Nanobiomedical Research

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The fi ndings and conclusions in this chapter have not been formally disseminated by the Food and Drug Administration and should not be construed to represent any Agency determination or policy. The mention of commercial products, their sources, or their use in connection with material reported herein is not to be construed as either an actual or implied endorsement of such products by the Department of Health and Human Services.The word "nanotechnology" confers images of extremely small objects that are very precisely engineered to perform targeted and complex tasks, by virtue of their small size. While this notion might be accurate for electronics and sensor nanotechnology applications, the progress of nanomedicine development is not as advanced as in other fields. Although, there are, at present, examples of marketed drug products containing nanoscale materials, one cannot say that drug development has been revolutionized by the advent of Handbook of Nanobiomedical Research Downloaded from www.worldscientific.com by CHINESE UNIVERSITY OF HONG KONG on 12/27/14. For personal use only.

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Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery

Cited by 96 publications

References 17 publications

Peningkatan Laju Disolusi Dispersi Padat Amorf Genistein dengan PVP K-30

Peningkatan Laju Disolusi Dispersi Padat Amorf Genistein dengan PVP K-30

Nanopreparations for Oral Administration

Biological Requirement and Safety Assessment of Nanomedicines

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