The Effect of the Particle Size Reduction on the Biorelevant Solubility and Dissolution of Poorly Soluble Drugs with Different Acid-Base Character

Author:

Csicsák Dóra1,Szolláth Rita1,Kádár Szabina2,Ambrus Rita3ORCID,Bartos Csilla3ORCID,Balogh Emese4,Antal István4ORCID,Köteles István1ORCID,Tőzsér Petra2,Bárdos Vivien1,Horváth Péter1ORCID,Borbás Enikő2,Takács-Novák Krisztina1,Sinkó Bálint5,Völgyi Gergely1ORCID

Affiliation:

1. Department of Pharmaceutical Chemistry, Semmelweis University, 9 Hőgyes Endre Street, 1092 Budapest, Hungary

2. Department of Organic Chemistry and Technology, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, 3 Műegyetem Rkp., 1111 Budapest, Hungary

3. Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, 6 Eötvös Street, 6720 Szeged, Hungary

4. Department of Pharmaceutics, Semmelweis University, 7 Hőgyes Endre Street, 1092 Budapest, Hungary

5. Pion Inc., 10 Cook Street, Billerica, MA 01821, USA

Abstract

Particle size reduction is a commonly used process to improve the solubility and the dissolution of drug formulations. The solubility of a drug in the gastrointestinal tract is a crucial parameter, because it can greatly influence the bioavailability. This work provides a comprehensive investigation of the effect of the particle size, pH, biorelevant media and polymers (PVA and PVPK-25) on the solubility and dissolution of drug formulations using three model compounds with different acid-base characteristics (papaverine hydrochloride, furosemide and niflumic acid). It was demonstrated that micronization does not change the equilibrium solubility of a drug, but it results in a faster dissolution. In contrast, nanonization can improve the equilibrium solubility of a drug, but the selection of the appropriate excipient used for nanonization is essential, because out of the two used polymers, only the PVPK-25 had an increasing effect on the solubility. This phenomenon can be explained by the molecular structure of the excipients. Based on laser diffraction measurements, PVPK-25 could also inhibit the aggregation of the particles more effectively than PVA, but none of the polymers could hold the nanonized samples in the submicron range until the end of the measurements.

Funder

National Research, Development, and Innovation Fund of Hungary

New National Excellence program of the Ministry for Innovation and Technology

Publisher

MDPI AG

Subject

Pharmaceutical Science

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