Oral nanotherapeutics with enhanced mucus penetration and ROS-responsive drug release capacities for delivery of curcumin to colitis tissues

2020 ◽  
Author(s):  
Yamei Huang ◽  
Brandon Canup ◽  
Shuangquan Gou ◽  
Nanxi Chen ◽  
Fangyin Dai ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Mucus Penetration

The therapeutic efficacies of oral nanotherapeutics for ulcerative colitis (UC) are seriously hindered by the lack of mucus-penetrating capacity and uncontrolled drug release. To overcome these limitations, the surface of...

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

scholarly journals Formulation and evaluation of Prednisolone retention enema as dispersible tablet and vehicle for the treatment of ulcerative colitis

2019 ◽  
Vol 8 (2) ◽  
pp. 545-552
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Evaluation Studies ◽  
Wet Granulation ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Retention Enema ◽  
Dispersible Tablet ◽  
Dispersible Tablets

Ulcerative colitis is a chronic idiopathic inflammatory bowel disease that causes chronic inflammation and damage in the gastrointestinal (GI) tract that typically presents in the second or third decade of life with bloody diarrhoea and abdominal cramps. The objective of the present work was to formulate and evaluate of Prednisolone retention enema as a dispersible tablet and it is suspended in suitable vehicle for the treatment of ulcerative colitis. In the present work, an attempt has been made to formulate and evaluate Prednisolone retention enema as a dispersible tablet by using three different methods (direct compression (F1 to F3, wet granulation (F4 and F5) and slugging method (F6)). Prepared dispersible tablets were administered with the help of vehicle for the effective treatment of ulcerative colitis. Dispersible tablets were evaluated for various parameters. In vitro drug release and microbiological evaluation studies were performed to the best formulation in rectal suspension. Then the best formulation was subjected to carry out for stability studies at three different temperatures. Among the six formulations, F6 formulation showed better results. FT-IR study showed that there was no interaction between a drug and excipients. In vitro drug release and microbiological evaluation studies were performed for F6 formulation in rectal suspension. About 99.06 % of the drug was released at 60 min. and also it was found to be microbiologically stable. Results from the stability studies showed that F6 formulation alone and with rectal suspension was stable for a period of 90 days. It was concluded that F6 formulation in rectal suspension possesses a promising future for the treatment of ulcerative colitis.

scholarly journals Design and Evaluation of Colon Specific Delivery of Budesonide Core in Coat Matrix Tablet Used In Local Ulcerative Colitis

2016 ◽  
Vol 8 (02) ◽  
Author(s):  
Mallikarjuna M. ◽  
Ramakrishna A.
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Cecal Content ◽  
S 100

In the present investigation planned to study the less explored sterculia gum as matrix carrier of Budesonide to colon. Developed the formulations from B1 to B4 contains alone sterculia gum and its proportion increased gradually in the formulation. The formulations B5 to B10 contain the sterculia gum in combination with Eudragit S 100 and the hydrophilic, hydrophobic polymer. The budesonide core in coat matrix tablets was prepared by direct compression method. The powder bed of the formulations is evaluated for pre compressional characteristics like bulk density, tapped density, compressibility index and angle of repose. The compressed budesonide core in coat matrix tablets were evaluated for post compressional characteristics like thickness, diameter, hardness, disintegration, friability and to understand the drug release pattern and to correlate the in vivo condition, the in vitro dissolution performed in three different gastro intestinal pH at 1.2, pH 7.4 and pH 6.8 with and without 4% rat cecal content. The in vitro dissolution results of formulations ascertain that sterculia gum alone in formulation uncontrolled the drug release in first 5 hrs and carried lesser amount of drug to colon. The formulations B8 in the first 5 hours released 4.3% and carried the larger amount of drug to colon and in absence of rat cecal content released 90% and in presences of 4% rat cecal content released 99% of drug, indicating the sterculia gum undergoes enzymatic degradation and this formulation is considered as potential in targeting the budesonide to colon in the local ulcerative colitis

Design, Formulation and Characterization of Microspheres containing Mesalamine for the Treatment of Ulcerative Colitis

2021 ◽  
pp. 165-169
Author(s):  
Deepak Patel ◽  
Sunil Kumar Shah ◽  
Chandra Kishore Tyagi
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Simulated Gastric Fluid ◽  
Simulated Intestinal Fluid ◽  
Chitosan Microspheres ◽  
Increase With Increase

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72% - 82.27%, drug loading from 20.28% - 33.26%. The size of the prepared microspheres ranged between 61.22-90.41μm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. The release profile of mesalamine from eudragit-coated chitosan micro-spheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.

scholarly journals Colon specific drug delivery of mesalamine using eudragit S100-coated chitosan microspheres for the treatment of ulcerative colitis

2013 ◽  
Vol 2 (3) ◽  
pp. 42-48 ◽  
Author(s):  
Seema Badhana ◽  
Navneet Garud ◽  
Akanksha Garud
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Simulated Gastric Fluid ◽  
Chitosan Microspheres ◽  
Increase With Increase ◽  
Eudragit S100

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72%-82.27%, drug loading from 20.28%-33.26%. The size of the prepared microspheres ranged between 61.22-90.41µm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. Micromeritic properties showed good flow properties and packability of prepared microspheres. The drug release of mesalamine from microspheres was found to decrease as the polymer concentration increases. The release profile of mesalamine from eudragit-coated chitosan microspheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.DOI: http://dx.doi.org/10.3329/icpj.v2i3.13577 International Current Pharmaceutical Journal, February 2013, 2(3): 42-48 

Mannan-binding lectin gene polymorphisms in ulcerative colitis and Crohn's disease

2001 ◽  
Vol 120 (5) ◽  
pp. A459-A459
Author(s):  
A RECTOR ◽  
P LEMEY ◽  
W LAFFUT ◽  
E KEYAERTS ◽  
F STRUYF ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Crohn’S Disease ◽  
Crohn's Disease ◽  
Gene Polymorphisms ◽  
Lectin Gene ◽  
Mannan Binding Lectin ◽  
Binding Lectin
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