Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2015 Jun 23:9:3231-8.
doi: 10.2147/DDDT.S86458. eCollection 2015.

Design of a gelatin microparticle-containing self-microemulsifying formulation for enhanced oral bioavailability of dutasteride

In-hwan Baek  1 , Eun-Sol Ha  2 , Jin-Wook Yoo  2 , Yunjin Jung  2 , Min-Soo Kim  2
Affiliations

Design of a gelatin microparticle-containing self-microemulsifying formulation for enhanced oral bioavailability of dutasteride

In-hwan Baek et al. Drug Des Devel Ther. .

Abstract

In this study, a gelatin microparticle-containing self-microemulsifying formulation (SMF) was developed using a spray-drying method to enhance the oral delivery of the poorly water-soluble therapeutic dutasteride. The effect of the amount of gelatin and the type and amount of hydrophilic additives, namely, Gelucire(®) 44/14, poloxamer 407, sodium lauryl sulfate, Soluplus(®), Solutol™ HS15, and D-α-tocopheryl polyethylene glycol 1000 succinate, on the droplet size, dissolution, and oral absorption of dutasteride from the SMF was investigated. Upon dispersion of the gelatin microparticle-containing SMF in water after spray-drying, the mean droplet size of the aqueous dispersion was in the range of 110-137 nm. The in vitro dissolution and recrystallization results showed that gelatin could be used as a solid carrier and recrystallization inhibitor for the SMF of dutasteride. Furthermore, combination of the gelatin microparticle-containing SMF and Soluplus enhanced the dissolution properties and oral absorption of dutasteride. The results of our study suggest that the gelatin microparticle-containing SMF in combination with Soluplus could be useful to enhance the oral absorption of dutasteride.

Keywords: bioavailability; dissolution; dutasteride; solubility.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Scanning electron micrographs of gelatin microparticle-containing self-microemulsifying formulations of dutasteride. (A) G3 particles and (B) G13 particles.
Figure 2
Figure 2
Effect of gelatin on dissolution profiles of gelatin microparticle-containing self-microemulsifying formulations of dutasteride. Note: Data are expressed as the mean ± standard deviation (n=4).
Figure 3
Figure 3
Effect of gelatin on dissolution profiles of gelatin microparticle-containing self-microemulsifying formulations of dutasteride. Note: Data are expressed as the mean ± standard deviation (n=4).
Figure 4
Figure 4
Effect of surfactant on dissolution profiles of gelatin microparticle-containing self-microemulsifying formulations of dutasteride. Note: Data are expressed as the mean ± standard deviation (n=4).
Figure 5
Figure 5
Effect of Soluplus® on dissolution profiles of gelatin microparticle-containing self-microemulsifying formulations of dutasteride. Note: Data are expressed as the mean ± standard deviation (n=4).
Figure 6
Figure 6
Effect of type of dissolution medium on dissolution profiles of gelatin microparticle-containing self-microemulsifying formulation of dutasteride (G13). Note: Data are expressed as the mean ± standard deviation (n=4).
Figure 7
Figure 7
Plasma concentration–time profiles of dutasteride in rats after oral administration of gelatin microparticle-containing self-microemulsifying formulations. Note: Data are expressed as the mean ± standard deviation (n=5).
See this image and copyright information in PMC

References

    1. Sprunk A, Strachan CJ, Graf A. Rational formulation development and in vitro assessment of SMEDDS for oral delivery of poorly water soluble drugs. Eur J Pharm Sci. 2012;46:508–515. - PubMed
    1. Cho W, Kim MS, Kim JS, et al. Optimized formulation of solid self-microemulsifying sirolimus delivery systems. Int J Nanomedicine. 2013;8:1673–1682. - PMC - PubMed
    1. Pandey S, Das U, Patil A. Formulation and ex-vivo evaluation of metronidazole microemulsion loaded hydrogel for prevention of periodontitis. J Pharm Invest. 2014;44:225–236.
    1. Yadav P, Yadav E, Verma A, Amin S. In vitro characterization and pharmacodynamic evaluation of furosemide loaded self nano emulsifying drug delivery system (SNEDDS) J Pharm Invest. 2014;44:443–453.
    1. Tang B, Cheng G, Gu JC, Xu CH. Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms. Drug Discov Today. 2008;13:606–612. - PubMed

Publication types

MeSH terms