Enteric polymers beyond protection: mechanistic insights and translational implications for supersaturating oral drug delivery systems
5 affiliations
- 1Chartwell Pharmaceuticals LLC, 77 Brenner Dr, Congers, NY, 10920, USA
- 2Department of Pharmaceutical Chemistry, College of Pharmacy, JSS University, Noida, Uttar Pradesh, 201301, India
- 3Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research -Ahmedabad (NIPER-A), Palaj, Gandhinagar, Gujarat, 382355, India
- 4Intas Pharmaceuticals, Ahmedabad, Gujarat, 380054, India
- 5Department of Pharmacology, College of Pharmacy, JSS University, Noida, Uttar Pradesh, 201301, India
Abstract
Poor aqueous solubility continues to limit oral delivery of many drugs. Weak bases are particularly challenging because they may dissolve in the stomach and subsequently precipitate as the gastrointestinal pH increases. Enteric polymers are therefore being explored not only as protective coatings but also as functional carriers in amorphous solid dispersions (ASDs). This review looks at enteric polymers from the perspective of spatiotemporal regulation of supersaturation, encompassing where drug release begins and what happens to the drug after release. The discussion covers HPMCAS, HPMCP, and methacrylate-based polymers including Eudragit L100-55, Eudragit L100, and Kollicoat MAE 100-55. Published studies on drug release, precipitation, phase behavior, membrane transport, and pharmacokinetics are considered together with regulatory information for selected marketed products. Enteric polymers do not produce uniform effects across formulations. Depending on the drug, polymer grade, drug loading, dissolution conditions, and manufacturing process, they may modulate gastric drug release, influence pH-shift precipitation, and affect nucleation, crystal growth, or drug-rich colloidal phases. However, increased apparent drug concentration does not necessarily indicate a greater concentration of molecularly dissolved drug, membrane transport, or systemic exposure. The review also considers manufacturing-related factors, including spray drying and hot-melt extrusion, and outlines a mechanism-based framework for selecting enteric polymers according to drug-specific biopharmaceutical risks, drug-polymer compatibility, and practical development requirements. Overall, enteric polymers should be selected based on formulation-specific evidence rather than the assumption that pH-dependent release will inherently improve oral bioavailability.
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BibTeX
@article{joshi2026enteric,
title = {{Enteric polymers beyond protection: mechanistic insights and translational implications for supersaturating oral drug delivery systems}},
author = {Vishvesh Joshi and Lokesh Yadav and Yalamanda Varla and Pranav Patel and Yagni Shah and Arvee Prajapati and Vijaykumar Chaudhary and Rikin Patel and Praveen Thaggikuppe Krishnamurthy and Sonam Patel and Derajram Benival},
journal = {International journal of pharmaceutics: X},
year = {2026},
month = oct,
doi = {10.1016/j.ijpx.2026.100689},
url = {https://europepmc.org/article/PMC/PMC13717165},
note = {CC BY},
}
RIS
TY - JOUR
TI - Enteric polymers beyond protection: mechanistic insights and translational implications for supersaturating oral drug delivery systems
AU - Vishvesh Joshi
AU - Lokesh Yadav
AU - Yalamanda Varla
AU - Pranav Patel
AU - Yagni Shah
AU - Arvee Prajapati
AU - Vijaykumar Chaudhary
AU - Rikin Patel
AU - Praveen Thaggikuppe Krishnamurthy
AU - Sonam Patel
AU - Derajram Benival
PY - 2026
DA - 2026/10/17
JO - International journal of pharmaceutics: X
DO - 10.1016/j.ijpx.2026.100689
UR - https://europepmc.org/article/PMC/PMC13717165
AB - Poor aqueous solubility continues to limit oral delivery of many drugs. Weak bases are particularly challenging because they may dissolve in the stomach and subsequently precipitate as the gastrointestinal pH increases. Enteric polymers are therefore being explored not only as protective coatings but also as functional carriers in amorphous solid dispersions (ASDs). This review looks at enteric polymers from the perspective of spatiotemporal regulation of supersaturation, encompassing where drug release begins and what happens to the drug after release. The discussion covers HPMCAS, HPMCP, and methacrylate-based polymers including Eudragit L100-55, Eudragit L100, and Kollicoat MAE 100-55. Published studies on drug release, precipitation, phase behavior, membrane transport, and pharmacokinetics are considered together with regulatory information for selected marketed products. Enteric polymers do not produce uniform effects across formulations. Depending on the drug, polymer grade, drug loading, dissolution conditions, and manufacturing process, they may modulate gastric drug release, influence pH-shift precipitation, and affect nucleation, crystal growth, or drug-rich colloidal phases. However, increased apparent drug concentration does not necessarily indicate a greater concentration of molecularly dissolved drug, membrane transport, or systemic exposure. The review also considers manufacturing-related factors, including spray drying and hot-melt extrusion, and outlines a mechanism-based framework for selecting enteric polymers according to drug-specific biopharmaceutical risks, drug-polymer compatibility, and practical development requirements. Overall, enteric polymers should be selected based on formulation-specific evidence rather than the assumption that pH-dependent release will inherently improve oral bioavailability.
SN - 2590-1567
ER -