Preactivated thiomers: Permeation enhancing properties

Wang, Xueqing; Iqbal, Javed; Rahmat, Deni; Bernkop‐Schnürch, Andreas

doi:10.1016/j.ijpharm.2012.08.045

Cited by 39 publications

(20 citation statements)

References 24 publications

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“…Results from in vitro permeation studies displayed the permeation enhancement ability for preactivated thiomers and was ranked as follows: PAA(450)-Cys-2MNA (h) >PAA(250)-Cys-2MNA (h) > PAA(100)-Cys-2MNA (h) on both Caco-2 cells and rat intestinal mucosa. Also, the apparent permeability of sodium fluorescein was observed to be 5.08-fold higher in Caco-2 cells for PAA(450)-Cys-2MNA (h) and 2.46-fold higher on intestinal mucosa for PAA(450)-Cys-2MNA (m), respectively, relative to sodium fluorescein in buffer only (Wang et al, 2012). Such enhancement in permeability as well as better stability render preactivated thiomers as promising macromolecular permeation enhancers and mucoadhesive polymers and may be suitable for non-invasive drug administration.…”

Section: Formulation Strategies For Increasing the Oral Bioavailabmentioning

confidence: 95%

Approaches for enhancing oral bioavailability of peptides and proteins

Renukuntla

Vadlapudi

Patel

et al. 2013

International Journal of Pharmaceutics

563

331

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Oral delivery of peptide and protein drugs faces immense challenge partially due to the gastrointestinal (GI) environment. In spite of considerable efforts by industrial and academic laboratories, no major breakthrough in the effective oral delivery of polypeptides and proteins has been accomplished. Upon oral administration, gastrointestinal epithelium acts as a physical and biochemical barrier for absorption of proteins resulting in low bioavailability (typically less than 1–2%). An ideal oral drug delivery system should be capable of a) maintaining the integrity of protein molecules until it reaches the site of absorption, b) releasing the drug at the target absorption site, where the delivery system appends to that site by virtue of specific interaction, and c) retaining inside the gastrointestinal tract irrespective of its transitory constraints. Various technologies have been explored to overcome the problems associated with the oral delivery of macromolecules such as insulin, gonadotropin-releasing hormones, calcitonin, human growth factor, vaccines, enkephalins, and interferons, all of which met with limited success. This review article intends to summarize the physiological barriers to oral delivery of peptides and proteins and novel pharmaceutical approaches to circumvent these barriers and enhance oral bioavailability of these macromolecules.

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Section: Formulation Strategies For Increasing the Oral Bioavailabmentioning

confidence: 95%

Approaches for enhancing oral bioavailability of peptides and proteins

Renukuntla

Vadlapudi

Patel

et al. 2013

International Journal of Pharmaceutics

563

331

View full text Add to dashboard Cite

show abstract

“…The reactive form of thiomers is the thiolate anion, whereas the p K a of alkyl thiols is in the range of 8–10, meaning thiomers will be most reactive in a pH range slightly above the physiological pH. As a consequence, their full potential is not extended in mucosal delivery . To overwhelm these limitations, preactivated thiomers bearing an additional ligand with a heteroaromatic structure reacting in a pH‐independent manner were designed and evaluated within this study.…”

Section: Introductionmentioning

confidence: 99%

“…As a consequence, their full potential is not extended in mucosal delivery. 8 To overwhelm these limitations, preactivated thiomers bearing an additional ligand with a heteroaromatic structure reacting in a pH-independent manner were designed and evaluated within this study.…”

Section: Introductionmentioning

confidence: 99%

Chemical Modification of Hyaluronic Acid for Intraoral Application

Laffleur

Röggla

Idrees

et al. 2014

Journal of Pharmaceutical Sciences

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“…As HA-MNA exhibits totally protected S-groups, it is not necessary to perform the dialysis in acidic environment. As reported in Another synthetic path for the synthesis of S-protected polymers was proposed previously (Wang, Iqbal, Rahmat & Bernkop-Schnürch, 2012). This procedure is based on the synthesis of the thiolated polymer followed by a reaction with MNA-MNA dimer.…”

Section: Synthesis Of Thiolated and Totally Protected Hyaluronic Acidmentioning

confidence: 99%

“…The amount of immobilized MNA was assessed as described byWang et al (Wang, Iqbal, Rahmat & Bernkop-Schnürch, 2012). The amount of unbound MNA was determined following the same procedure but without the addition of glutathione.3.5.…”

mentioning

confidence: 99%