Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon-specific delivery

Asghar, Laila Fatima Ali; Azeemuddin,; Jain, Varun; Chandran, Sajeev

doi:10.1080/10717540902823960

Cited by 6 publications

(4 citation statements)

References 40 publications

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“…Values of b were significantly greater than 1, indicating the sigmoid profile. A sigmoidal release profile characterized by slower release in the initial stage (0-1 h) followed by rapid release during the later stage (3-6 h) may ensure targeted drug release to the colon (Ali Asghar et al, 2009).…”

Section: In Vitro Drug Releasementioning

confidence: 99%

Evaluation of polyelectrolyte and emulsion covalent crosslink of chitosan for producing mesalasine loaded submicron particles

Lacerda

Piantino

Gonzaga

et al. 2019

Braz. J. Pharm. Sci.

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This study evaluates various techniques for producing mesalamine (5ASA)-loaded particles employing chitosan as a biopolymer: (1) the polyelectrolyte complexation of chitosan with phthalate hypromelose (HP), (2) the chemical crosslinking of chitosan with genipin and (3) the water-in-oil emulsion method associated with chemical crosslinking with genipin. Systems were characterized by dynamic light scattering, zeta potential (ζ), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and a drug release profile. Method (1) was efficiently produced unloaded nanoparticles (491 nm, PdI=0.26 and ζ = 23.2), but the conditions for chitosan and HP cross-linking enhanced the precipitation of 5ASA. Method (2) caused the degradation of the drug. Method 3 produced sub-micron and microparticles, thereby varying the agitation method; 3 h magnetic agitation resulted in 2692 nm, Pdi = 0.6 and ζ = 46, while Ultra-Turrax, 5 min produced submicron particles (537 nm, PdI = 0.6). The percentage yield was approximately 50%, which is very satisfactory considering the impossibility of encapsulating 5ASA using other methods. FTIR showed the covalent interaction of chitosan and genipin. The drug release was rapid in acidic fluid, but in neutral pH a slower release was obtained in the initial stage, followed by rapid release, which may ensure the controlled release of 5ASA in the colon.

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Section: In Vitro Drug Releasementioning

confidence: 99%

Evaluation of polyelectrolyte and emulsion covalent crosslink of chitosan for producing mesalasine loaded submicron particles

Lacerda

Piantino

Gonzaga

et al. 2019

Braz. J. Pharm. Sci.

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“…In-vitro drug release of formulation F2 tablets 17,18 From the in-vitro release studies, coated tablets show better release. It has released 55.2% of the drug was released at the end of 12 h (Figure 1).…”

Section: Disintegration Of Formulation F2 Tabletsmentioning

confidence: 99%

Polymeric Micelles of Capecitabine: Design, Characterization & Cytotoxic Study

Nayanika¹,

Subramanian²

2018

IJCTR

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The present study was aimed to prepare polymeric micelles of capecitabine: design, characterization & cytotoxic study. Capecitabine is a prodrug used in the treatment of metastatic colorectal cancer and breast cancer. Polymeric micelles formulations are being formulated to achieve smaller particle size, good stability, increase the solubility, and prolong release of the drug. The micelles have been prepared by using organic solvent/water emulsion technique. Then the prepared formulation has been undergone for drug content, entrapment efficiency, particles size, zeta potential. From this best formulation is converted into tablets by using the excipients. Preformulation study was carried out by using with and without excipients. Then tablets were made using direct compression method by using 9mm concave punches in rotary tablet press. Then the tablet is dip coated using ethyl cellulose of different concentrations. The formulations were evaluated for thickness, hardness, disintegration, dissolution. The tablets shows release formulation upto 12 h.Cytotoxic study has been done in human colon cancer (HT-29) cells by using MTT assay.

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“…To deliver antiinflammatory agents to the sites of inflammation, various drug delivery approaches have been developed, including pH-sensitive system, time-dependent system, pro-drugs, and microflora-activated system, and thus systemic drug absorption should be reduced, as this leads to unwanted systemic side effects [5][6][7] . The pH-sensitive system and the time-dependent system are the most commonly utilised systems for colon-specific medication delivery [8][9][10] . Polysaccharides are monosaccharide polymers with a variety of qualities.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Enteric Coated Matrix Tablets of Mesalamine for Inflammatory Bowel Disease

Chourey¹,

Chouksey²

2022

J. Drug Delivery Ther.

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Mesalamine is a gold standard anti-inflammatory drug used to treat inflammatory bowel illnesses. It's usually used to treat and keep Ulcerative Colitis in remission in mild to moderate cases. Mesalamine is rapidly cleared from circulation after being consumed orally, with an elimination half-life of only one hour. Oral intake of delayed or slow released matrix formulations can acquire therapeutic concentration in the intestines. The goal of this study was to use guar gum as a carrier to develop colon-specific delivery methods for mesalamine. The matrix tablets were made using the direct compression process, which is today regarded as a cost-effective and straightforward manufacturing method. Dip coating was used to coat the tablets with varied concentrations of Eudragit L100 polymer. Tablets were studied in vitro in a variety of dissolution solutions, including 0.1 N HCl (pH 1.2), phosphate buffers pH 6.8 and 7.4, and others. The optimized formulation was subjected to swelling tests. All of the formulations' physicochemical parameters were confirmed to be in line with pharmacopoeial norms. All formulations were subjected to stability tests in accordance with ICH recommendations. The tablets coated with Eudragit L100 (20 percent w/v) had a sustained release of 78.39 percent over 12 hours, while the uncoated tablets released the medication in 9 hours. Tablet stability tests revealed that under accelerated and room temperature storage settings for 6 months, there was reduced degradation. In the colon, the enteric-coated Eudragit L100 coated matrix tablets of mesalamine demonstrated promising site-specific drug delivery. Keywords: Mesalamine, Guar gum, Eudragit L100, Direct compression, Inflammatory bowel illnesses

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Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon-specific delivery

Abstract: (2009) Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon-specific delivery, Drug Delivery, 16:4,[205][206][207][208][209][210][211][212][213]

Cited by 6 publications

References 40 publications

Evaluation of polyelectrolyte and emulsion covalent crosslink of chitosan for producing mesalasine loaded submicron particles

Evaluation of polyelectrolyte and emulsion covalent crosslink of chitosan for producing mesalasine loaded submicron particles

Polymeric Micelles of Capecitabine: Design, Characterization & Cytotoxic Study

Formulation and Evaluation of Enteric Coated Matrix Tablets of Mesalamine for Inflammatory Bowel Disease

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