scholarly journals Highly Porous pH-Responsive Carboxymethyl Chitosan-Grafted-Poly (Acrylic Acid) Based Smart Hydrogels for 5-Fluorouracil Controlled Delivery and Colon Targeting

2019 ◽  
Vol 2019 ◽  
pp. 1-15 ◽  
Author(s):  
Samiullah Khan ◽  
Naveed Anwar

In the present investigation, new formulations of CMCS/AA hydrogels with varying composition of Carboxymethyl chitosan, acrylic acid, and ethylene glycol dimethacrylate (EGDMA) were prepared by free radical polymerization technique using benzoyl peroxide as catalyst. The bioavailability of 5-FU through the oral route is very limited owing to its rapid metabolism and clearance from the general circulation. Current work was aimed at increasing the bioavailability of 5-FU via smart hydrogels and at investigating their potential in delivering 5-FU to target colon cancer. Swelling studies were carried out on dried hydrogel discs in different USP phosphate buffer solutions of various pH values. Porosity and gel fraction of all the samples were measured. 5-FU was used as a model drug and loaded in selected hydrogel samples. The amount of drug loaded and released was determined. Experimental data was fitted to various model equations, and corresponding parameters were calculated to study the release mechanism. Many structural parameters were calculated. The prepared hydrogels were also characterized by FTIR and SEM to study the structure, crystallinity, compatibility, and morphology of the smart hydrogels. The biocompatibility and cytotoxic potential blank and drug-loaded hydrogels were assessed through MTT assay. The prepared hydrogels were found to be an excellent carrier for 5-FU in targeting colon cancer.

2015 ◽  
Vol 2015 ◽  
pp. 1-15 ◽  
Author(s):  
Syed Majid Hanif Bukhari ◽  
Samiullah Khan ◽  
Muhammad Rehanullah ◽  
Nazar Mohammad Ranjha

This present work was aimed at synthesizing pH-sensitive cross-linked AA/Gelatin hydrogels by free radical polymerization. Ammonium persulfate and ethylene glycol dimethacrylate (EGDMA) were used as initiator and as cross-linking agent, respectively. Different feed ratios of acrylic acid, gelatin, and EGDMA were used to investigate the effect of monomer, polymer, and degree of cross-linking on swelling and release pattern of the model drug. The swelling behavior of the hydrogel samples was studied in 0.05 M USP phosphate buffer solutions of various pH values pH 1.2, pH 5.5, pH 6.5, and pH 7.5. The prepared samples were evaluated for porosity and sol-gel fraction analysis. Pheniramine maleate used for allergy treatment was loaded as model drug in selected samples. The release study of the drug was investigated in 0.05 M USP phosphate buffer of varying pH values (1.2, 5.5, and 7.5) for 12 hrs. The release data was fitted to various kinetic models to study the release mechanism. Hydrogels were characterized by Fourier transformed infrared (FTIR) spectroscopy which confirmed formation of structure. Surface morphology of unloaded and loaded samples was studied by surface electron microscopy (SEM), which confirmed the distribution of model drug in the gel network.


Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.


2014 ◽  
Vol 22 (12) ◽  
pp. 1330-1336 ◽  
Author(s):  
Hossein Abdollahi ◽  
Vahid Najafi ◽  
Farshid Ziaee ◽  
Kourosh Kabiri ◽  
Farhad Narimani

2011 ◽  
Vol 31 (3) ◽  
pp. 677-682 ◽  
Author(s):  
Oscar D'Agostini-Junior ◽  
Carmen Lucia Petkowicz ◽  
Angelica Garcia Couto ◽  
Sergio Faloni de Andrade ◽  
Rilton Alves Freitas

2014 ◽  
Vol 50 (1) ◽  
pp. 173-184 ◽  
Author(s):  
Kashif Sohail ◽  
Ikram Ullah Khan ◽  
Yasser Shahzad ◽  
Talib Hussain ◽  
Nazar Muhammad Ranjha

In this study, we fabricated pH-sensitive polyvinylpyrrolidone/acrylic acid (PVP/AA) hydrogels by a free-radical polymerisation method with variation in the content of monomer, polymer and cross-linking agent. Swelling was performed in USP phosphate buffer solutions of pH 1.2, 5.5, 6.5 and 7.5 with constant ionic strength. Network structure was evaluated by different parameters and FTIR confirmed the formation of cross-linked hydrogels. X-ray crystallography showed molecular dispersion of tramadol HCl. A drug release study was carried out in phosphate buffer solutions of pH 1.2, 5.5 and 7.5 for selected samples. It was observed that swelling and drug release from hydrogels can be modified by changing composition and degree of cross-linking of the hydrogels under investigation. Swelling coefficient was high at higher pH values except for the one containing high PVP content. Drug release increased by increasing the pH of the medium and AA contents in hydrogels while increasing the concentration of cross-linking agent had the opposite effect. Analysis of the drug release mechanism revealed non-Fickian transport of tramadol from the hydrogels.


2012 ◽  
Vol 6 ◽  
pp. CMO.S8194 ◽  
Author(s):  
J. Quidde ◽  
D. Arnold ◽  
A. Stein

Large randomized trials demonstrated a benefit of adjuvant chemotherapy after resection of the primary colon cancer. It improves overall survival and reduces the risk of death, by 5% in UICC (Union Internationale Contre le Cancer) stage II and approximately 15%–20% in stage III. Fluoropyrimidines have been the standard drugs for the treatment of colon cancer since large randomized controlled trials demonstrated their efficacy and safety in treating patients suffering from this disease. Capecitabine is an orally administered fluoropyrimidine, which is preferably activated in tumor tissue to the active moiety 5-fluorouracil (5FU) and is cytotoxic through inhibition of DNA synthesis. It has proven equivalent efficacy and tolerability despite a changed toxicity profile compared to 5FU with less myelosuppression but more hand-and-foot syndrome. Capecitabine is well tolerated in elderly patients. The oral route of administration avoids frequent clinical visits as well as insertion of central venous catheters. The impact of the particular drug features on daily clinical practice is discussed in this review.


2005 ◽  
Vol 288-289 ◽  
pp. 129-132 ◽  
Author(s):  
Ling Chen ◽  
Xiao Xi Li ◽  
Lin Li ◽  
Bing Li

Colon-targeting drug delivery systems (CDDSs) are employed to improve the bioavailability of protein and peptide drugs through the oral route. So it is important to prepare the drug carriers for oral CDDS. In this study, the Enzyme-Resistant starch (RS) was studied for use as a vehicle in oral colon-targeting drug delivery. The characteristics of RS powders were investigated by X-ray diffraction, polarizing microscopy, DSC and SEM, and their film were examined by enzymatic digestion test. The results showed that RS could be a promising film-former for pharmaceutical coatings, having good stability to enzymatic digestion. Furthermore, a novel peroral formulation using RS coating and bovine serum albumin as a model drug was studied for colon-specific drug delivery in vitro. Drug release studies have shown that RS coating could delivery the drug to the colon and the release rate in simulated colonic fluids was dependent on the biodegradation of RS and its coatings. It is indicated that the RS coated tablet is a potential system for oral CDDS.


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