Back to Journals » International Journal of Nanomedicine » Volume 6

In situ formation of nanocrystals from a self-microemulsifying drug delivery system to enhance oral bioavailability of fenofibrate

Authors

Lin YM, Wu JU, Chen YC, Su YD, Ke WT, Ho HO, Sheu MT

Published 19 October 2011 Volume 2011:6 Pages 2445—2457

DOI https://doi.org/10.2147/IJN.S25339

Review by Single-blind

Peer reviewer comments 5

You-Meei Lin1, Jui-Yu Wu2, Ying-Chen Chen3, Yu-Der Su3, Wen-Tin Ke3, Hsiu-O Ho3
1Department of Pharmacy, Shuang Ho Hospital, 2Department of Biochemistry, School of Medicine, 3School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROC
Objectives: In situ formation of nanocrystals and dissolution profiles of fenofibrate (FFB) from a self-microemulsifying drug delivery system (SMEDDS) were characterized.
Methods: SMEDDS formulated with Myritol® and surfactant mixture (Smix) of D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and either Tween® 20 (A, C, E, G, M, S, N, T, O) or Tween® 80 (B, D, F, H, P, U, Q, V, R) at various oil/Smix ratios (Group I: A and B of 0.42, C and D of 0.25, E and F of 0.11; Group II: G and H of 1.38, M and P of 1.11, S and U of 0.9, N and Q of 0.73, T and V of 0.58, and O and R of 0.46) and water contents (1: 9.5%, 2: 5.0%, 3: 0.0%, G-V: 4.5%). Their dissolutions were conducted at different rotation speeds. Two optimal SMEDDSs containing Tween 80(B2) or a higher oil/Smix ratio(Q) and B2(solution) were selected for pharmacokinetic study.
Results: FFB particles formed within the nanosize range from Group I gradually increased with time but decreased with increasing stirring rates. However, the mean size of FFB formed by B series was as low as 200 nm, which was smaller than that of A series at three stirring rates. The release rate from both groups obviously increased with increasing stirring rate. However, incomplete release was observed for S and N in Tween 20 series, whereas a faster release rate and complete release were observed for Tween 80 series with an insignificant difference among them. Results of pharmacokinetic study demonstrated that the highest-ranked area under the curve and Cmax values were for Q(SMEDDS) and B2(solution), respectively. The relative bioavailability of Q(SMEDDS) with respect to Tricor® was enhanced by about 1.14-1.22-fold.
Conclusion: SMEDDS, consisting of Myritol 318 and TPGS combined with Tween 80 at 4:1, was able to enhance the oral bioavailability of FFB.
Keywords: SMEDDS, fenofibrate, microemulsion, dissolution, TPGS

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]

 

Other articles by this author:

Wound-healing effect of micronized sacchachitin (mSC) nanogel on corneal epithelium

Chen RN, Lee LW, Chen LC, Ho HO, Lui SC, Sheu MT, Su CH

International Journal of Nanomedicine 2012, 7:4697-4706

Published Date: 28 August 2012

Development of terbinafine solid lipid nanoparticles as a topical delivery system

Chen Y-C, Liu D-Z, Liu J-J, Chang T-W, Ho H-O, Sheu M-T

International Journal of Nanomedicine 2012, 7:4409-4418

Published Date: 15 August 2012

Readers of this article also read:

Green synthesis of water-soluble nontoxic polymeric nanocomposites containing silver nanoparticles

Prozorova GF, Pozdnyakov AS, Kuznetsova NP, Korzhova SA, Emel’yanov AI, Ermakova TG, Fadeeva TV, Sosedova LM

International Journal of Nanomedicine 2014, 9:1883-1889

Published Date: 16 April 2014

Methacrylic-based nanogels for the pH-sensitive delivery of 5-Fluorouracil in the colon

Ashwanikumar N, Kumar NA, Nair SA, Kumar GS

International Journal of Nanomedicine 2012, 7:5769-5779

Published Date: 15 November 2012

A novel preparation method for silicone oil nanoemulsions and its application for coating hair with silicone

Hu Z, Liao M, Chen Y, Cai Y, Meng L, Liu Y, Lv N, Liu Z, Yuan W

International Journal of Nanomedicine 2012, 7:5719-5724

Published Date: 12 November 2012

Cross-linked acrylic hydrogel for the controlled delivery of hydrophobic drugs in cancer therapy

Deepa G, Thulasidasan AK, Anto RJ, Pillai JJ, Kumar GS

International Journal of Nanomedicine 2012, 7:4077-4088

Published Date: 27 July 2012

Preparation and characterization of polysaccharide-based nanoparticles with anticoagulant activity

da Silva LC, Garcia T, Mori M, Sandri G, Bonferoni MC, Finotelli PV, Cinelli LP, Caramella C, Cabral LM

International Journal of Nanomedicine 2012, 7:2975-2986

Published Date: 18 June 2012

Synergistic enhancement of cancer therapy using a combination of docetaxel and photothermal ablation induced by single-walled carbon nanotubes

Wang L, Zhang MY, Zhang N, Shi JJ, Zhang HL, Li M, Lu C, Zhang ZZ

International Journal of Nanomedicine 2011, 6:2641-2652

Published Date: 31 October 2011

Crystallization after intravitreal ganciclovir injection

Pitipol Choopong, Nattaporn Tesavibul, Nattawut Rodanant

Clinical Ophthalmology 2010, 4:709-711

Published Date: 14 July 2010