The effects of primary unconjugated bile acids on nanoencapsulated pharmaceutical formulation of hydrophilic drugs: Pharmacological implications

Armin Mooranian, Thomas Foster, Corina M. Ionescu, Louise Carey, Daniel Walker, Melissa Jones, Susbin Raj Wagle, Bozica Kovacevic, Jacqueline Chester, Edan Johnstone, Jafri Kuthubutheen, Daniel Brown, Marcus D. Atlas, Momir Mikov, Hani Al-Salami

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)

Abstract

Introduction: In a recent study, in our laboratory, primary unconjugated bile acids, com-monly found in humans, chenodeoxycholic acid (CDCA), have been shown to improve stability of nanoencapsulated lipophilic drugs and improve their release profile after oral administration likely via electrokinetic stabilisation. Hence, this study aimed to examine the effects of CDCA on exerting similar effects on hydrophilic drugs. Methods: Various CDCA-based formulations were produced for the orally administered hydrophilic drug, metformin. Analyses of these formulations included electrokinetic potentials, topography, drug and CDCA formulation contents, nano size distribution, heat-induced deforma-tion and outer-core expansion indices, release profiles, shell-resistance ratio, and thermal and chemical indices. With the drug’s main target being pancreatic beta-cells, the formulations’ effects on cell viability, functions and inflammatory profiles were also investigated. Results and Conclusions: CDCA-based metformin formulations exhibited improved stability and release profiles via thermal, chemical and electrokinetic effects, which were formulation-dependent suggesting potential applications of CDCA in the oral targeted delivery of hydrophilic drugs.
Original languageEnglish
Pages (from-to)4423-4434
Number of pages12
JournalDrug Design, Development and Therapy
Volume15
DOIs
Publication statusPublished - Oct 2021
Externally publishedYes

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