Colon Targeted Drug Delivery Systems: A Review on Primary and Novel Approaches

Philip, Anil K.; Philip, Betty

doi:10.5001/omj.2010.24

Cited by 309 publications

(190 citation statements)

References 64 publications

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“…The pH of GIT changes and is always varying, but these three pH values have been used in many studies conducting preliminary and in vitro release tests to mimic the pH conditions of the GIT. A solution at pH 1.2 represents gastric fluid in the stomach, while buffer solutions at pH 6.8 and pH 7.4 simulate the jejunal region of small intestine and the ileum segment, respectively [20,23,39].…”

Section: Loading and In Vitro Release Kinetics Studymentioning

confidence: 99%

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Synthesis of Gelatin-γ-Polyglutamic Acid-Based Hydrogel for the In Vitro Controlled Release of Epigallocatechin Gallate (EGCG) from Camellia sinensis

et al. 2013

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Abstract:The antioxidant property and other health benefits of the most abundant catechin, epigallocatechin gallate (EGCG), are limited because of poor stability and permeability across intestine. Protecting the EGCG from the harsh gastrointestinal tract (GIT) environment can help to increase its bioavailability following oral administration. In this study, EGCG was loaded to hydrogel prepared from ionic interaction between an optimized concentration of gelatin and γ-polyglutamic acid (γ-PGA), with ethylcarbodiimide (EDC) as the crosslinker. Physicochemical characterization of hydrogel was done using Fourier transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The dependence of the swelling degree (SD) of the hydrogel to the amount of gelatin, γ-PGA, EDC, swelling time and pH was determined. A high SD of the crosslinked hydrogel was noted at pH 4.5, 6.8 OPEN ACCESSPolymers 2014, 6 40 and 9.0 compared to pH 7.4, which describes pH-responsiveness. Approximately 67% of the EGCG from the prepared solution was loaded to the hydrogel after 12 h post-loading, in which loading efficiency was related to the amount of EDC. The in vitro release profile of EGCG at pH 1.2, 6.8 and 7.4, simulating GIT conditions, resulted in different sustained release curves. Wherein, the released EGCG was not degraded instantly compared to free-EGCG at controlled temperature of 37 °C at different pH monitored against time. Therefore, this study proves the potential of pH-responsive gelatin-γ-PGA-based hydrogel as a biopolymer vehicle to deliver EGCG.

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Section: Loading and In Vitro Release Kinetics Studymentioning

confidence: 99%

“…The release of EGCG was done in three pH levels of solution, such as 1.2, 6.8 and 7.4, to act as GIT fluids, specifically simulating gastric fluid, the jejunal region of small intestine and the ileum segment, respectively [23]. Approximately, 0.1 M HCl was used to make pH 1.2, while PBS was used to for pH 6.8 and 7.4.…”

Section: In Vitro Egcg Release Kineticsmentioning

confidence: 99%

Synthesis of Gelatin-γ-Polyglutamic Acid-Based Hydrogel for the In Vitro Controlled Release of Epigallocatechin Gallate (EGCG) from Camellia sinensis

et al. 2013

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“…Therefore, chitosan derivatives with enhanced solubility at basic and neutral pH are essential. [12][13][14][15] It has been shown that TMC, a quaternary derivative of chitosan, enhances penetration and opens epithelial tight junctions in the environments with basic and neutral pH. 14 The gastric enzymes and acidic conditions pose challenges to the oral administration of vaccines.…”

Section: Introductionmentioning

confidence: 99%

Enteric trimethyl chitosan nanoparticles containing hepatitis B surface antigen for oral delivery

Farhadian

Dounighi

Avadi³

2015

Human Vaccines & Immunotherapeutics

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Oral vaccination is the preferred route of immunization. However, the degradative condition of the gastrointestinal tract and the higher molecular size of peptides pose major challenges in developing an effective oral vaccination system. One of the most excellent methods used in the development of oral vaccine delivery system relies on the entrapment of the antigen in polymeric nanoparticles. In this work, trimethyl chitosan (TMC) nanoparticles were fabricated using ionic gelation teqnique by interaction hydroxypropyl methylcellulose phthalate (HPMCP), a pHsensitive polymer, with TMC and the utility of the particles in the oral delivery of hepatitis B surface antigen (HBsAg) was evaluated employing solutions that simulated gastric and intestinal conditions. The particle size, morphology, zeta potential, loading capacity, loading efficiency, in vitro release behavior, structure, and morphology of nanoparticles were evaluated, and the activity of the loaded antigen was assessed. Size of the optimized TMC/HPMCP nanoparticles and that of the antigen-loaded nanoparticles were 85 nm and 158 nm, respectively. Optimum loading capacity (76.75%) and loading efficiency (86.29%) were achieved at 300 mg/mL concentration of the antigen. SEM images revealed a spherical shape as well as a smooth and near-homogenous surface of nanoparticles. Results of the in vitro release studies showed that formulation with HPMCP improved the acid stability of the TMC nanoparticles as well as their capability to preserve the loaded HBsAg from gastric destruction. The antigen showed good activity both before and after loading. The results suggest that TMC/HPMCP nanoparticles could be used in the oral delivery of HBsAg vaccine.

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“…Inside the human colon, numerous bacteria secrete enzymes that break down the polymer backbone, resulting in decrease in its molecular weight, thus losing their mechanical strength and ending up with the release of drug entity. Besides pectin, CS is also able to shield drugs from harsh stomach and small intestine environment [33]. A successful colon drug delivery requires the triggering mechanism in the delivery system that only responds to the physiological conditions particular to the colon [34].…”

Section: In Vitro Drugmentioning

confidence: 99%

Cell Growth Inhibition Effect of DsiRNA Vectorised by Pectin-Coated Chitosan-Graphene Oxide Nanocomposites as Potential Therapy for Colon Cancer

Katas

Amin

Moideen

et al. 2017

Journal of Nanomaterials

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Colonic-targeted drug delivery system is widely explored to combat colon-related diseases such as colon cancer. Dicer-substrate small interfering RNA (DsiRNA) has been explored for cancer therapy due to its potency in targeting specific gene of interest. However, its application is limited by rapid degradation and poor cellular uptake. To address this, chitosan-graphene oxide (CS-GO) nanocomposite was used to deliver DsiRNA effectively into cells. Additionally, pectin was used as compatibilization agent to allow specific delivery to the colon and protect the nanocomposites from the harsh environment in the stomach and small intestine. CS-GO-DsiRNA nanocomposites were prepared by electrostatic interaction between CS and GO prior to coating with pectin. The mean particle size of CS-GO-DsiRNA-pectin nanocomposites was 554.5 ± 124.6 nm with PDI and zeta potential of 0.47 ± 0.19 and −10.7 ± 3.0 mV, respectively. TEM analysis revealed smooth and spherical shape of CS-GO-DsiRNA nanocomposites and the shape became irregular after pectin coating. FTIR analysis further confirmed the successful formation of CS-GO-DsiRNApectin nanocomposites. Furthermore, the nanocomposites were able to entrap high amount of DsiRNA (% entrapment efficiency of 92.6 ± 3.9%) with strong binding efficiency. CS-GO-DsiRNA-pectin nanocomposites also selectively inhibited cell growth of colon cancer cell line (Caco-2 cells) and were able to decrease VEGF level significantly. In a nutshell, pectin-coated DsiRNA-loaded CS-GO nanocomposites were successfully developed and they have a great potential to deliver DsiRNA to the colon effectively.

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Colon Targeted Drug Delivery Systems: A Review on Primary and Novel Approaches

Cited by 309 publications

References 64 publications

Synthesis of Gelatin-γ-Polyglutamic Acid-Based Hydrogel for the In Vitro Controlled Release of Epigallocatechin Gallate (EGCG) from Camellia sinensis

Synthesis of Gelatin-γ-Polyglutamic Acid-Based Hydrogel for the In Vitro Controlled Release of Epigallocatechin Gallate (EGCG) from Camellia sinensis

Enteric trimethyl chitosan nanoparticles containing hepatitis B surface antigen for oral delivery

Cell Growth Inhibition Effect of DsiRNA Vectorised by Pectin-Coated Chitosan-Graphene Oxide Nanocomposites as Potential Therapy for Colon Cancer

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