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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.


Related in: MedlinePlus

In vitro release profiles of different mesalamine formulations.Notes: Release experiments were carried out in 0.1 N HCl (2 hours), PBS at pH 7.4 (3 hours), and PBS at pH 6.8 (20 hours), at 37°C±0.5°C. Each point represents the mean value of three different experiments ± SD. ×, mesalamine-coated microparticles; Δ, mesalamine suspensions; n=3.Abbreviations: PBS, phosphate-buffered saline; SD, standard deviation.
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f2-dddt-10-2021: In vitro release profiles of different mesalamine formulations.Notes: Release experiments were carried out in 0.1 N HCl (2 hours), PBS at pH 7.4 (3 hours), and PBS at pH 6.8 (20 hours), at 37°C±0.5°C. Each point represents the mean value of three different experiments ± SD. ×, mesalamine-coated microparticles; Δ, mesalamine suspensions; n=3.Abbreviations: PBS, phosphate-buffered saline; SD, standard deviation.

Mentions: Release profiles of mesalamine-coated microparticles and mesalamine suspensions are illustrated in Figure 2. It was noticed that the release rate of mesalamine-coated microparticles was significantly lower than that of mesalamine suspensions. Approximately 100% of drug in suspensions was released within 5 hours, suggesting a burst release effect in suspensions and indicating that nearly all the drug was released before they reached colon. However, mesalamine-coated microparticles showed a completely different release curve. The initial release phase did not show a burst release and the drug released from the coated microparticles was low. A small amount of drug was detected in HCl at a pH of 1.2 and PBS medium at a pH 7.4 of for 5 hours, which indicates that the release of drug was suppressed by the “burst effect” to some extent. Only 3.2%±0.4% of drug was released after 5 hours. Then 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. The mesalamine release profile was prominently prolonged by the encapsulation of coated microparticles.


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)

In vitro release profiles of different mesalamine formulations.Notes: Release experiments were carried out in 0.1 N HCl (2 hours), PBS at pH 7.4 (3 hours), and PBS at pH 6.8 (20 hours), at 37°C±0.5°C. Each point represents the mean value of three different experiments ± SD. ×, mesalamine-coated microparticles; Δ, mesalamine suspensions; n=3.Abbreviations: PBS, phosphate-buffered saline; SD, standard deviation.
© Copyright Policy
Related In: Results  -  Collection

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

f2-dddt-10-2021: In vitro release profiles of different mesalamine formulations.Notes: Release experiments were carried out in 0.1 N HCl (2 hours), PBS at pH 7.4 (3 hours), and PBS at pH 6.8 (20 hours), at 37°C±0.5°C. Each point represents the mean value of three different experiments ± SD. ×, mesalamine-coated microparticles; Δ, mesalamine suspensions; n=3.Abbreviations: PBS, phosphate-buffered saline; SD, standard deviation.
Mentions: Release profiles of mesalamine-coated microparticles and mesalamine suspensions are illustrated in Figure 2. It was noticed that the release rate of mesalamine-coated microparticles was significantly lower than that of mesalamine suspensions. Approximately 100% of drug in suspensions was released within 5 hours, suggesting a burst release effect in suspensions and indicating that nearly all the drug was released before they reached colon. However, mesalamine-coated microparticles showed a completely different release curve. The initial release phase did not show a burst release and the drug released from the coated microparticles was low. A small amount of drug was detected in HCl at a pH of 1.2 and PBS medium at a pH 7.4 of for 5 hours, which indicates that the release of drug was suppressed by the “burst effect” to some extent. Only 3.2%±0.4% of drug was released after 5 hours. Then 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. The mesalamine release profile was prominently prolonged by the encapsulation of coated microparticles.

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.


Related in: MedlinePlus