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Article

Enhancing Dissolution and Oral Bioavailability of Ursodeoxycholic Acid with a Spray-Dried pH-Modified Extended Release Formulation

1
BK21 FOUR Community-Based Intelligent Novel Drug Discovery Education Unit, Vessel-Organ Interaction Research Center (VOICE), Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, Daegu 41566, Korea
2
College of Pharmacy, Dankook University, Cheonan-si 31116, Korea
*
Author to whom correspondence should be addressed.
Academic Editor: Peter Timmins
Pharmaceutics 2022, 14(5), 1037; https://doi.org/10.3390/pharmaceutics14051037
Received: 22 March 2022 / Revised: 24 April 2022 / Accepted: 9 May 2022 / Published: 11 May 2022
(This article belongs to the Special Issue Feature Papers in Physical Pharmacy and Formulation)
Ursodeoxycholate (UDCA) has low oral bioavailability and pH-dependent solubility and permeability. Thus, we developed a pH-modified extended-release formulation of UDCA using Na2CO3 as the alkalizing agent and hydroxypropyl methylcellulose (HPMC) as the release-modifying agent. The optimized pH-modified controlled-release UDCA formulation, with the UDCA:HPMC:Na2CO3 ratio of 200:600:150 (w/w/w), was prepared using a spray-drying method. Then, the formulation’s solubility, dissolution, and pharmacokinetic properties were characterized. In a pH-modified extended-release formulation of UDCA, the solubility of UDCA was increased to 8 mg/mL with a sustained dissolution for 12 h. Additionally, the spray-dried formulation exhibited amorphous states without molecular interaction among UDCA, Na2CO3, and HPMC. Moreover, the plasma UDCA concentration of the formulation maintained a higher UDCA concentration for up to 48 h than that of UDCA itself or the non-extended-release UDCA formulation. Consequently, the formulation significantly increased the AUC compared to UDCA or the non-extended-release UDCA formulation in rats. In conclusion, we have improved UDCA’s solubility and dissolution profile by preparing a pH-modified extended-release formulation with the UDCA:HPMC:Na2CO3 ratio of 200:600:150 (w/w/w), which effectively increased the oral bioavailability of UDCA by 251% in rats. View Full-Text
Keywords: ursodeoxycholate (UDCA); oral bioavailability; pH-modified extended release formulation; spray-drying method ursodeoxycholate (UDCA); oral bioavailability; pH-modified extended release formulation; spray-drying method
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MDPI and ACS Style

Lee, J.; Lee, C.H.; Lee, J.-G.; Jeon, S.Y.; Choi, M.-K.; Song, I.-S. Enhancing Dissolution and Oral Bioavailability of Ursodeoxycholic Acid with a Spray-Dried pH-Modified Extended Release Formulation. Pharmaceutics 2022, 14, 1037. https://doi.org/10.3390/pharmaceutics14051037

AMA Style

Lee J, Lee CH, Lee J-G, Jeon SY, Choi M-K, Song I-S. Enhancing Dissolution and Oral Bioavailability of Ursodeoxycholic Acid with a Spray-Dried pH-Modified Extended Release Formulation. Pharmaceutics. 2022; 14(5):1037. https://doi.org/10.3390/pharmaceutics14051037

Chicago/Turabian Style

Lee, Jaehyeok, Chul H. Lee, Jong-Geon Lee, So Y. Jeon, Min-Koo Choi, and Im-Sook Song. 2022. "Enhancing Dissolution and Oral Bioavailability of Ursodeoxycholic Acid with a Spray-Dried pH-Modified Extended Release Formulation" Pharmaceutics 14, no. 5: 1037. https://doi.org/10.3390/pharmaceutics14051037

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