Time-Based Formulation Strategies for Colon Drug Delivery
Despite poor absorption properties, delivery to the colon of bioactive compounds administered by the oral route has become a focus of pharmaceutical research over the last few decades. In particular, the high prevalence of Inflammatory Bowel Disease has driven interest because of the need for improv...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-12-01
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| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/14/12/2762 |
| _version_ | 1797455752674148352 |
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| author | Andrea Gazzaniga Saliha Moutaharrik Ilaria Filippin Anastasia Foppoli Luca Palugan Alessandra Maroni Matteo Cerea |
| author_facet | Andrea Gazzaniga Saliha Moutaharrik Ilaria Filippin Anastasia Foppoli Luca Palugan Alessandra Maroni Matteo Cerea |
| author_sort | Andrea Gazzaniga |
| collection | DOAJ |
| description | Despite poor absorption properties, delivery to the colon of bioactive compounds administered by the oral route has become a focus of pharmaceutical research over the last few decades. In particular, the high prevalence of Inflammatory Bowel Disease has driven interest because of the need for improved pharmacological treatments, which may provide high local drug concentrations and low systemic exposure. Colonic release has also been explored to deliver orally biologics having gut stability and permeability issues. For colon delivery, various technologies have been proposed, among which time-dependent systems rely on relatively constant small intestine transit time. Drug delivery platforms exploiting this physiological feature provide a lag time programmed to cover the entire small intestine transit and control the onset of release. Functional polymer coatings or capsule plugs are mainly used for this purpose, working through different mechanisms, such as swelling, dissolution/erosion, rupturing and/or increasing permeability, all activated by aqueous fluids. In addition, enteric coating is generally required to protect time-controlled formulations during their stay in the stomach and rule out the influence of variable gastric emptying. In this review, the rationale and main delivery technologies for oral colon delivery based on the time-dependent strategy are presented and discussed. |
| first_indexed | 2024-03-09T15:58:52Z |
| format | Article |
| id | doaj.art-eb8dc215158b46c1ba4e6f7dfb54f0cd |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T15:58:52Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-eb8dc215158b46c1ba4e6f7dfb54f0cd2023-11-24T17:21:35ZengMDPI AGPharmaceutics1999-49232022-12-011412276210.3390/pharmaceutics14122762Time-Based Formulation Strategies for Colon Drug DeliveryAndrea Gazzaniga0Saliha Moutaharrik1Ilaria Filippin2Anastasia Foppoli3Luca Palugan4Alessandra Maroni5Matteo Cerea6Sezione di Tecnologia e Legislazione Farmaceutiche “Maria Edvige Sangalli”, GazzaLaB, Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via G. Colombo 71, 20133 Milano, ItalySezione di Tecnologia e Legislazione Farmaceutiche “Maria Edvige Sangalli”, GazzaLaB, Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via G. Colombo 71, 20133 Milano, ItalySezione di Tecnologia e Legislazione Farmaceutiche “Maria Edvige Sangalli”, GazzaLaB, Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via G. Colombo 71, 20133 Milano, ItalySezione di Tecnologia e Legislazione Farmaceutiche “Maria Edvige Sangalli”, GazzaLaB, Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via G. Colombo 71, 20133 Milano, ItalySezione di Tecnologia e Legislazione Farmaceutiche “Maria Edvige Sangalli”, GazzaLaB, Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via G. Colombo 71, 20133 Milano, ItalySezione di Tecnologia e Legislazione Farmaceutiche “Maria Edvige Sangalli”, GazzaLaB, Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via G. Colombo 71, 20133 Milano, ItalySezione di Tecnologia e Legislazione Farmaceutiche “Maria Edvige Sangalli”, GazzaLaB, Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via G. Colombo 71, 20133 Milano, ItalyDespite poor absorption properties, delivery to the colon of bioactive compounds administered by the oral route has become a focus of pharmaceutical research over the last few decades. In particular, the high prevalence of Inflammatory Bowel Disease has driven interest because of the need for improved pharmacological treatments, which may provide high local drug concentrations and low systemic exposure. Colonic release has also been explored to deliver orally biologics having gut stability and permeability issues. For colon delivery, various technologies have been proposed, among which time-dependent systems rely on relatively constant small intestine transit time. Drug delivery platforms exploiting this physiological feature provide a lag time programmed to cover the entire small intestine transit and control the onset of release. Functional polymer coatings or capsule plugs are mainly used for this purpose, working through different mechanisms, such as swelling, dissolution/erosion, rupturing and/or increasing permeability, all activated by aqueous fluids. In addition, enteric coating is generally required to protect time-controlled formulations during their stay in the stomach and rule out the influence of variable gastric emptying. In this review, the rationale and main delivery technologies for oral colon delivery based on the time-dependent strategy are presented and discussed.https://www.mdpi.com/1999-4923/14/12/2762colon targetingtime-controlled releasepulsatile releasetime-dependent releasesmall intestinal transit timein vivo human data |
| spellingShingle | Andrea Gazzaniga Saliha Moutaharrik Ilaria Filippin Anastasia Foppoli Luca Palugan Alessandra Maroni Matteo Cerea Time-Based Formulation Strategies for Colon Drug Delivery Pharmaceutics colon targeting time-controlled release pulsatile release time-dependent release small intestinal transit time in vivo human data |
| title | Time-Based Formulation Strategies for Colon Drug Delivery |
| title_full | Time-Based Formulation Strategies for Colon Drug Delivery |
| title_fullStr | Time-Based Formulation Strategies for Colon Drug Delivery |
| title_full_unstemmed | Time-Based Formulation Strategies for Colon Drug Delivery |
| title_short | Time-Based Formulation Strategies for Colon Drug Delivery |
| title_sort | time based formulation strategies for colon drug delivery |
| topic | colon targeting time-controlled release pulsatile release time-dependent release small intestinal transit time in vivo human data |
| url | https://www.mdpi.com/1999-4923/14/12/2762 |
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