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A nanomedicine-promising approach to provide an appropriate colon-targeted drug delivery system for 5-fluorouracil.

Singh S, Kotla NG, Tomar S, Maddiboyina B, Webster TJ, Sharma D, Sunnapu O - Int J Nanomedicine (2015)

Bottom Line: Targeted drug delivery plays a significant role in disease treatment associated with the colon, affording therapeutic responses for a prolonged period of time with low side effects.In vitro results obtained from these experiments indicated the successful targeted delivery of 5-fluorouracil to the colon.In vivo results conclude a practical mechanism to maintain the integrity and intactness of the intestinal/colonic microflora, in the face of a "chemical attack" by oral colon-targeted drug delivery for colon cancer treatment.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.

ABSTRACT
Targeted drug delivery plays a significant role in disease treatment associated with the colon, affording therapeutic responses for a prolonged period of time with low side effects. Colorectal cancer is the third most common cancer in both men and women with an estimated 102,480 cases of colon cancer and 40,340 cases of rectal cancer in 2013 as reported by the American Cancer Society. In the present investigation, we developed an improved oral delivery system for existing anticancer drugs meant for colon cancer via prebiotic and probiotic approaches. The system comprises three components, namely, nanoparticles of drug coated with natural materials such as guar gum, xanthan gum (that serve as prebiotics), and probiotics. The natural gums play a dual role of protecting the drug in the gastric as well as intestinal conditions to allow its release only in the colon. In vitro results obtained from these experiments indicated the successful targeted delivery of 5-fluorouracil to the colon. Electron microscopy results demonstrated that the prepared nanoparticles were spherical in shape and 200 nm in size. The in vitro release data indicated that the maximum release occurs at pH 7.2 and 7.4 with 93% of the drug released in the presence of 4% (w/v) of rat cecal content. In vivo results conclude a practical mechanism to maintain the integrity and intactness of the intestinal/colonic microflora, in the face of a "chemical attack" by oral colon-targeted drug delivery for colon cancer treatment.

No MeSH data available.


Related in: MedlinePlus

Mean percentage of 5-fluorouracil released from nanoformulations (all values are mean ± SEM; n=3).Abbreviations: SEM, standard error of the mean; 5-FU, 5-fluorouracil.
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f2-ijn-10-7175: Mean percentage of 5-fluorouracil released from nanoformulations (all values are mean ± SEM; n=3).Abbreviations: SEM, standard error of the mean; 5-FU, 5-fluorouracil.

Mentions: The in vitro drug release study was carried out for 24 hours. The mean in vitro drug release showed that only 5% of the drug was released after 5 hours under simulated gastric and intestinal fluids. The percentage of drug released after a 6-hour wash increased (17%) in the presence of cecal content. After 24 hours, the percentage of cumulative amount of 5-FU released in the presence of cecal content was found to be 93%. It is evident from the results that the 5-FU-loaded nanoparticles were successful in retarding the initial drug release in other parts of the gastrointestinal tract except the colon as shown in Figure 2.


A nanomedicine-promising approach to provide an appropriate colon-targeted drug delivery system for 5-fluorouracil.

Singh S, Kotla NG, Tomar S, Maddiboyina B, Webster TJ, Sharma D, Sunnapu O - Int J Nanomedicine (2015)

Mean percentage of 5-fluorouracil released from nanoformulations (all values are mean ± SEM; n=3).Abbreviations: SEM, standard error of the mean; 5-FU, 5-fluorouracil.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4664497&req=5

f2-ijn-10-7175: Mean percentage of 5-fluorouracil released from nanoformulations (all values are mean ± SEM; n=3).Abbreviations: SEM, standard error of the mean; 5-FU, 5-fluorouracil.
Mentions: The in vitro drug release study was carried out for 24 hours. The mean in vitro drug release showed that only 5% of the drug was released after 5 hours under simulated gastric and intestinal fluids. The percentage of drug released after a 6-hour wash increased (17%) in the presence of cecal content. After 24 hours, the percentage of cumulative amount of 5-FU released in the presence of cecal content was found to be 93%. It is evident from the results that the 5-FU-loaded nanoparticles were successful in retarding the initial drug release in other parts of the gastrointestinal tract except the colon as shown in Figure 2.

Bottom Line: Targeted drug delivery plays a significant role in disease treatment associated with the colon, affording therapeutic responses for a prolonged period of time with low side effects.In vitro results obtained from these experiments indicated the successful targeted delivery of 5-fluorouracil to the colon.In vivo results conclude a practical mechanism to maintain the integrity and intactness of the intestinal/colonic microflora, in the face of a "chemical attack" by oral colon-targeted drug delivery for colon cancer treatment.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.

ABSTRACT
Targeted drug delivery plays a significant role in disease treatment associated with the colon, affording therapeutic responses for a prolonged period of time with low side effects. Colorectal cancer is the third most common cancer in both men and women with an estimated 102,480 cases of colon cancer and 40,340 cases of rectal cancer in 2013 as reported by the American Cancer Society. In the present investigation, we developed an improved oral delivery system for existing anticancer drugs meant for colon cancer via prebiotic and probiotic approaches. The system comprises three components, namely, nanoparticles of drug coated with natural materials such as guar gum, xanthan gum (that serve as prebiotics), and probiotics. The natural gums play a dual role of protecting the drug in the gastric as well as intestinal conditions to allow its release only in the colon. In vitro results obtained from these experiments indicated the successful targeted delivery of 5-fluorouracil to the colon. Electron microscopy results demonstrated that the prepared nanoparticles were spherical in shape and 200 nm in size. The in vitro release data indicated that the maximum release occurs at pH 7.2 and 7.4 with 93% of the drug released in the presence of 4% (w/v) of rat cecal content. In vivo results conclude a practical mechanism to maintain the integrity and intactness of the intestinal/colonic microflora, in the face of a "chemical attack" by oral colon-targeted drug delivery for colon cancer treatment.

No MeSH data available.


Related in: MedlinePlus