Publicou 6 edições por ano
ISSN Imprimir: 0743-4863
ISSN On-line: 2162-660X
Indexed in
Oral Absorption Promoters: Opportunities, Issues, and Challenges
RESUMO
Transport of a drug across the biological membrane of the gastrointestinal tract has turned out to be a critical barrier against the success of any oral drug delivery technology. The unique advantages of the oral route, along with need for an oral substitute of invasive parenteral formulations and the reduction of intersubject variability in plasma profiles, has been an incentive for the use of excipients with absorption-enhancing properties to boost the bioavailability of poorly absorbed drugs. The development of such excipients is not a simple task, so understanding enhancement mechanisms in relation to physiology can facilitate the identification of structure−function relationships as well as the development of newer agents for customary applications. The literature is replete with reports of absorption promoters, the selection of which is influenced by the mechanisms, safety, pharmacological inertness, rapidity of action, reversibility of induced membrane alterations and excipient compatibility. Despite promising results in preliminary screenings, the development process is hindered by low reproducible efficacy and pharmacologically driven safety issues. In this review, we elaborate on the importance of permeation enhancers in oral drug delivery, their current status, and issues at the forefront of the development of formulations using absorption promoter technologies.
-
Bu Pengli, Narayanan Silpa, Dalrymple Damon, Cheng Xingguo, Serajuddin Abu T.M., Cytotoxicity assessment of lipid-based self-emulsifying drug delivery system with Caco-2 cell model: Cremophor EL as the surfactant, European Journal of Pharmaceutical Sciences, 91, 2016. Crossref
-
Xu Jin, Lin Yiqing, Boulas Pierre, Peterson Matthew L., Low colonic absorption drugs: risks and opportunities in the development of oral extended release products, Expert Opinion on Drug Delivery, 15, 2, 2018. Crossref
-
Navarro del Hierro Joaquín, Herrera Teresa, Fornari Tiziana, Reglero Guillermo, Martin Diana, The gastrointestinal behavior of saponins and its significance for their bioavailability and bioactivities, Journal of Functional Foods, 40, 2018. Crossref
-
Danielsen E. Michael, Hansen Gert H., Intestinal surfactant permeation enhancers and their interaction with enterocyte cell membranes in a mucosal explant system, Tissue Barriers, 5, 3, 2017. Crossref
-
Gómez Elena Cutrín, Anguiano Igea Soledad, Gómez Amoza José Luis, Otero Espinar Francisco J., Evaluation of the promoting effect of soluble cyclodextrins in drug nail penetration, European Journal of Pharmaceutical Sciences, 117, 2018. Crossref
-
Danielsen E., Hansen Gert, Probing the Action of Permeation Enhancers Sodium Cholate and N-dodecyl-β-D-maltoside in a Porcine Jejunal Mucosal Explant System, Pharmaceutics, 10, 4, 2018. Crossref
-
Corazza Fúlvio G., Ernesto Julia V., Nambu Felipe A.N., de Carvalho Luma R., Leite-Silva Vânia R., Varca Gustavo H.C., Calixto Leandro A., Vieira Daniel P., Andréo-Filho Newton, Lopes Patricia S., Papain-cyclodextrin complexes as an intestinal permeation enhancer: Permeability and in vitro safety evaluation, Journal of Drug Delivery Science and Technology, 55, 2020. Crossref
-
Barrera María G., Tejada Guillermo, Leonardi Darío, Lamas María C., Salomón Claudio J., A Novel Prototype Device for Microencapsulation of Benznidazole: In Vitro/In Vivo Studies, AAPS PharmSciTech, 21, 3, 2020. Crossref
-
Babadi Delaram, Dadashzadeh Simin, Osouli Mahraz, Daryabari Maryam Sadat, Haeri Azadeh, Nanoformulation strategies for improving intestinal permeability of drugs: A more precise look at permeability assessment methods and pharmacokinetic properties changes, Journal of Controlled Release, 321, 2020. Crossref
-
Gamboa Alexander, Schüßler Nina, Soto-Bustamante Eduardo, Romero-Hasler Patricio, Meinel Lorenz, Morales Javier O., Delivery of ionizable hydrophilic drugs based on pharmaceutical formulation of ion pairs and ionic liquids, European Journal of Pharmaceutics and Biopharmaceutics, 156, 2020. Crossref
-
Li Wanqiong, Zhu Xueqin, Zhou Xiuman, Wang Xiaoxi, Zhai Wenjie, Li Bingyu, Du Jiangfeng, Li Guodong, Sui Xinghua, Wu Yahong, Zhai Mingxia, Qi Yuanming, Chen Guanyu, Gao Yanfeng, An orally available PD-1/PD-L1 blocking peptide OPBP-1-loaded trimethyl chitosan hydrogel for cancer immunotherapy, Journal of Controlled Release, 334, 2021. Crossref
-
Danielsen E. Michael, Intestinal permeation enhancers: Lessons learned from studies using an organ culture model, Biochimica et Biophysica Acta (BBA) - Biomembranes, 1863, 1, 2021. Crossref