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Thiomers and their potential applications in drug delivery
被引:18
|作者:
Shah, Kifayat Ullah
[1
]
Shah, Shefaat Ullah
[2
,3
]
Dilawar, Naz
[1
]
Khan, Gul Majid
[1
]
Gibaud, Stephane
[3
]
机构:
[1] Quaid i Azam Univ, Dept Pharm, Islamabad, Pakistan
[2] Gomal Univ, Dept Pharmaceut, Fac Pharm, Dera Ismail Khan, Pakistan
[3] Univ Lorraine, Fac Pharm, CITHEFOR EA3452, 5 Rue Albert Lebrun, F-54000 Nancy, France
关键词:
Mucoadhesion;
oral delivery;
preactivated thiomers;
S-nitrosothiomers;
thiomers;
IN-VITRO EVALUATION;
PROTECTED THIOLATED CHITOSAN;
EFFLUX TRANSPORTER ACTIVITY;
PREACTIVATED THIOMERS;
HYALURONIC-ACID;
VIVO EVALUATION;
ORAL DELIVERY;
PHYSIOLOGICAL CONDITIONS;
RHEOLOGICAL EVALUATION;
POLY(ACRYLIC ACID);
D O I:
10.1080/17425247.2016.1227787
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
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.
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页码:601 / 610
页数:10
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