Introduction: Thiomers are the product of the immobilization of sulfhydryl-bearing ligands onto the polymer backbone of a conventional polymer, which results in a significant improvement in mucoadhesion; in situ gelation and efflux inhibition compare with unchanged polymers. Because of thiol groups, thiomers have more reactivity and enhanced protection against oxidation. Since the late 1990s, extensive work has been conducted on these promising polymeric excipients in the pharmaceutical field. Areas covered: This review covers thiomers, their classification and their different properties. Various techniques for the synthesis, purification and characterization of thiomers are described in detail. This review also encompasses their various properties such as mucoadhesion, permeation enhancement, in situ gelation and efflux inhibition, as well as different formulations based on thiomers. In addition to the use of thiomers as multifunctional excipients, this review also encompasses their use as drugs. Expert opinion: The synthesis is realized by linkage of sulfhydryl-bearing ligands but reported methods give low yields. Higher degrees of modification are not necessary and would probably lead to extreme changes in properties. Nevertheless, an accurate characterization of the final product is important. The scale-up procedure for industrial manufacturing has been adapted to produce GMP materials; Lacrimera (R) eye drops have already entered the European market.
机构:
Fudan Univ, Sch Pharm, Key Lab Smart Drug Delivery MOE, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Key Lab Smart Drug Delivery MOE, Shanghai 201203, Peoples R China
Lin, Hewei
Han, Rongze
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Fudan Univ, Sch Pharm, Key Lab Smart Drug Delivery MOE, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Key Lab Smart Drug Delivery MOE, Shanghai 201203, Peoples R China
Han, Rongze
Wu, Wei
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Fudan Univ, Sch Pharm, Key Lab Smart Drug Delivery MOE, Shanghai 201203, Peoples R China
Tongji Univ, Sch Med, Shanghai Skin Dis Hosp, Shanghai 200443, Peoples R China
Fudan Univ, Shanghai Pudong Hosp, Pudong Med Ctr, Ctr Med Res & Innovat, Shanghai 201399, Peoples R China
Fudan Zhangjiang Inst, Shanghai 201203, Peoples R ChinaFudan Univ, Sch Pharm, Key Lab Smart Drug Delivery MOE, Shanghai 201203, Peoples R China
机构:
Hebrew Univ Jerusalem, Fac Med, Sch Pharm, Inst Drug Res, IL-91120 Jerusalem, IsraelHebrew Univ Jerusalem, Fac Med, Sch Pharm, Inst Drug Res, IL-91120 Jerusalem, Israel
Ainbinder, D.
Paolino, D.
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Magna Graecia Univ Catanzaro, Dept Expt & Clin Med, Fac Med, I-88100 Germaneto, CZ, ItalyHebrew Univ Jerusalem, Fac Med, Sch Pharm, Inst Drug Res, IL-91120 Jerusalem, Israel
Paolino, D.
Fresta, M.
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Magna Graecia Univ Catanzaro, Fac Pharm, Dept Pharmacobiol Sci, I-88100 Germaneto, CZ, ItalyHebrew Univ Jerusalem, Fac Med, Sch Pharm, Inst Drug Res, IL-91120 Jerusalem, Israel
Fresta, M.
Touitou, E.
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Hebrew Univ Jerusalem, Fac Med, Sch Pharm, Inst Drug Res, IL-91120 Jerusalem, IsraelHebrew Univ Jerusalem, Fac Med, Sch Pharm, Inst Drug Res, IL-91120 Jerusalem, Israel
机构:
Univ Calif Berkeley, San Francisco, CA 94158 USA
UCSF Grad Program Bioengn, San Francisco, CA 94158 USAUniv Calif Berkeley, San Francisco, CA 94158 USA
Walsh, Laura A.
Allen, Jessica L.
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Univ Calif San Francisco, Dept Bioengn & Therapeut Sci, San Francisco, CA 94158 USAUniv Calif Berkeley, San Francisco, CA 94158 USA
Allen, Jessica L.
Desai, Tejal A.
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Univ Calif San Francisco, Dept Bioengn & Therapeut Sci, San Francisco, CA 94158 USAUniv Calif Berkeley, San Francisco, CA 94158 USA
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Univ Beira Interior, CICS UBI Hlth Sci Res Ctr, P-6200506 Covilha, Portugal
Polytechn Inst Guarda, Res Unit Inland Dev, CPIRN UDI IPG Ctr Potential & Innovat Nat Resourc, Ave Dr Francisco Sa Carneiro 50, P-6300559 Guarda, PortugalUniv Beira Interior, CICS UBI Hlth Sci Res Ctr, P-6200506 Covilha, Portugal