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Impact of Intestina...
Impact of Intestinal Concentration and Colloidal Structure on the Permeation-Enhancing Efficiency of Sodium Caprate in the Rat
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- Berg, Staffan (författare)
- Uppsala universitet,Institutionen för farmaci,AstraZeneca, R&D, Pharmaceut Sci, Adv Drug Delivery, S-43183 Gothenburg, Sweden.
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- Karrberg, Lillevi (författare)
- AstraZeneca, Biopharmaceut R&D, Clin Pharmacol & Safety Sci, Anim Sci & Technol, S-43183 Gothenburg, Sweden.
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- Suljovic, Denny (författare)
- Uppsala universitet,Institutionen för farmaci
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- Seeliger, Frank (författare)
- AstraZeneca, BioPharmaceut R&D, Clin Pharmacol & Safety Sci, Cardiovasc Renal & Metab Safety, S-43183 Gothenburg, Sweden.
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- Söderberg, Magnus (författare)
- AstraZeneca, BioPharmaceut R&D, Clin Pharmacol & Safety Sci, Cardiovasc Renal & Metab Safety, S-43183 Gothenburg, Sweden.
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- Perez-Alcazar, Marta (författare)
- AstraZeneca, Biopharmaceut R&D, Clin Pharmacol & Safety Sci, Imaging & Data Analyt, S-43183 Gothenburg, Sweden.
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- Van Zuydam, Natalie (författare)
- AstraZeneca, BioPharmaceut R&D, Discovery Sci, Data Sci & Quantitat Biol, S-43183 Gothenburg, Sweden.
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- Abrahamsson, Bertil (författare)
- AstraZeneca, Operat, Pharmaceut Technol & Dev, Oral Prod Dev, S-43183 Gothenburg, Sweden.
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- Hugerth, Andreas M. (författare)
- Ferring Pharmaceut AS, Global Pharmaceut R&D, DK-2300 Copenhagen, Denmark.
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- Davies, Nigel (författare)
- AstraZeneca, R&D, Pharmaceut Sci, Adv Drug Delivery, S-43183 Gothenburg, Sweden.
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- Bergström, Christel, 1973- (författare)
- Uppsala universitet,Institutionen för farmaci
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(creator_code:org_t)
- 2021-12-20
- 2022
- Engelska.
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Ingår i: Molecular Pharmaceutics. - : American Chemical Society (ACS). - 1543-8384 .- 1543-8392. ; 19:1, s. 200-212
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- In this work, we set out to better understand how the permeation enhancer sodium caprate (C10) influences the intestinal absorption of macromolecules. FITC-dextran 4000 (FD4) was selected as a model compound and formulated with 50-300 mM C10. Absorption was studied after bolus instillation of liquid formulation to the duodenum of anesthetized rats and intravenously as a reference, whereafter plasma samples were taken and analyzed for FD4 content. It was found that the AUC and C-max of FD4 increased with increasing C10 concentration. Higher C10 concentrations were associated with an increased and extended absorption but also increased epithelial damage. Depending on the C10 concentration, the intestinal epithelium showed significant recovery already at 60-120 min after administration. At the highest studied C10 concentrations (100 and 300 mM), the absorption of FD4 was not affected by the colloidal structures of C10, with similar absorption obtained when C10 was administered as micelles (pH 8.5) and as vesicles (pH 6.5). In contrast, the FD4 absorption was lower when C10 was administered at 50 mM formulated as micelles as compared to vesicles. Intestinal dilution of C10 and FD4 revealed a trend of decreasing FD4 absorption with increasing intestinal dilution. However, the effect was smaller than that of altering the total administered C10 dose. Absorption was similar when the formulations were prepared in simulated intestinal fluids containing mixed micelles of bile salts and phospholipids and in simple buffer solution. The findings in this study suggest that in order to optimally enhance the absorption of macromolecules, high (>= 100 mM) initial intestinal C10 concentrations are likely needed and that both the concentration and total dose of C10 are important parameters.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Nyckelord
- sodium caprate
- permeation enhancer
- FITC-dextran 4000
- oral peptide delivery
- rat intestinal instillation model
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Berg, Staffan
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Karrberg, Lillev ...
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Suljovic, Denny
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Seeliger, Frank
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Söderberg, Magnu ...
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Perez-Alcazar, M ...
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Van Zuydam, Nata ...
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Abrahamsson, Ber ...
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Hugerth, Andreas ...
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Davies, Nigel
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Bergström, Chris ...
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