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A novel pH-enzyme-dependent mesalamine colon-specific delivery system.

Jin L, Ding YC, Zhang Y, Xu XQ, Cao Q - Drug Des Devel Ther (2016)

Bottom Line: In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation.The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05).Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

View Article: PubMed Central - PubMed

Affiliation: Department of Gastroenterology, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.

ABSTRACT
The aim of the present study was to design a new pH-enzyme double-dependent mesalamine colon-specific delivery system. The drug release behaviors in vitro and pharmacokinetics and biodistribution in vivo were further evaluated. The mean particle diameters of mesalamine-coated microparticles were 312.2 µm. In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. A greater area under the plasma concentration-time curve (AUC)0-t was obtained for the coated microparticles (1.9-fold) compared to the suspensions group, which indicated that the encapsulated mesalamine had mostly been absorbed in rats over the period of 12 hours. The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05). Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

No MeSH data available.


The images of hematoxylin and eosin staining tissue sections of mice after intragastric administration of mesalamine-coated microparticles and mesalamine suspensions.Notes: Mesalamine-coated microparticles: (A) stomach, (B) small intestine, and (C) colon. Mesalamine suspensions: (D) stomach, (E) small intestine, and (F) colon. Magnification, ×500.
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f5-dddt-10-2021: The images of hematoxylin and eosin staining tissue sections of mice after intragastric administration of mesalamine-coated microparticles and mesalamine suspensions.Notes: Mesalamine-coated microparticles: (A) stomach, (B) small intestine, and (C) colon. Mesalamine suspensions: (D) stomach, (E) small intestine, and (F) colon. Magnification, ×500.

Mentions: In vivo, mesalamine-coated microparticles are thought to have the potential to maintain the concentration of mesalamine in the target range for a long time, reduce the influence caused by fluctuations in the concentrations of adverse, ensure the efficiency of treatment and reduce the frequency of administration, and improve patient compliance. In case of targeted drug-delivery system such as coated microparticles, a large portion of the drug and excipient is accumulated in specific tissues and, therefore, evaluating the compatibility between the tissues and formulations becomes a necessity to ensure the safety of the formulations. The cell structure of the tissue did not show any significant difference (degenerative changes) compared to the coated microparticles preparations and placebo group. Based on this observation, it was concluded that no histological changes were observed in the organs after the administration of mesalamine-coated microparticles (Figure 5).


A novel pH-enzyme-dependent mesalamine colon-specific delivery system.

Jin L, Ding YC, Zhang Y, Xu XQ, Cao Q - Drug Des Devel Ther (2016)

The images of hematoxylin and eosin staining tissue sections of mice after intragastric administration of mesalamine-coated microparticles and mesalamine suspensions.Notes: Mesalamine-coated microparticles: (A) stomach, (B) small intestine, and (C) colon. Mesalamine suspensions: (D) stomach, (E) small intestine, and (F) colon. Magnification, ×500.
© Copyright Policy
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4920224&req=5

f5-dddt-10-2021: The images of hematoxylin and eosin staining tissue sections of mice after intragastric administration of mesalamine-coated microparticles and mesalamine suspensions.Notes: Mesalamine-coated microparticles: (A) stomach, (B) small intestine, and (C) colon. Mesalamine suspensions: (D) stomach, (E) small intestine, and (F) colon. Magnification, ×500.
Mentions: In vivo, mesalamine-coated microparticles are thought to have the potential to maintain the concentration of mesalamine in the target range for a long time, reduce the influence caused by fluctuations in the concentrations of adverse, ensure the efficiency of treatment and reduce the frequency of administration, and improve patient compliance. In case of targeted drug-delivery system such as coated microparticles, a large portion of the drug and excipient is accumulated in specific tissues and, therefore, evaluating the compatibility between the tissues and formulations becomes a necessity to ensure the safety of the formulations. The cell structure of the tissue did not show any significant difference (degenerative changes) compared to the coated microparticles preparations and placebo group. Based on this observation, it was concluded that no histological changes were observed in the organs after the administration of mesalamine-coated microparticles (Figure 5).

Bottom Line: In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation.The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05).Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

View Article: PubMed Central - PubMed

Affiliation: Department of Gastroenterology, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.

ABSTRACT
The aim of the present study was to design a new pH-enzyme double-dependent mesalamine colon-specific delivery system. The drug release behaviors in vitro and pharmacokinetics and biodistribution in vivo were further evaluated. The mean particle diameters of mesalamine-coated microparticles were 312.2 µm. In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. A greater area under the plasma concentration-time curve (AUC)0-t was obtained for the coated microparticles (1.9-fold) compared to the suspensions group, which indicated that the encapsulated mesalamine had mostly been absorbed in rats over the period of 12 hours. The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05). Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

No MeSH data available.