Development of colon targeted multiparticulate pulsatile drug delivery system for treating nocturnal asthma

Kadam, Vinayak D.; Gattani, Surendra G.

doi:10.3109/10717541003762821

Cited by 29 publications

(17 citation statements)

References 26 publications

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“…However, using polymer micelles for oral drug delivery of macromolecular drugs (such as peptides, proteins, nucleic acids and sugars) is still fairly new and presents a major challenge because the human gastrointestinal tract resists the absorption of peptides, proteins, nucleic acids and other large molecules unless they are broken down into smaller molecules. [129][130][131] To optimize the oral delivery of biological macromolecules, various approaches have been pursued, including protective coatings [132][133][134] to protect the peptides during transport through the highly acidic environment in the stomach, targeted delivery, permeation enhancers, protease inhibitors, 135 and bioadhesive microparticles. [136][137][138] Nagasaki and coworkers designed reactive oxygen species (ROS) responsive nanoparticles (RNPO) for oral chemotherapy.…”

Section: Oral Delivery Routesmentioning

confidence: 99%

Polymeric nanoparticles for colon cancer therapy: overview and perspectives

et al. 2016

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Section: Oral Delivery Routesmentioning

confidence: 99%

Polymeric nanoparticles for colon cancer therapy: overview and perspectives

et al. 2016

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“…The colon specific drug delivery systems would also be used to treat the circadian diseases that have peak symptoms in the early morning, such as nocturnal asthma, as CDDS could bring about time delay for drug absorption, which is desirable from a therapeutic point of view (9). So by developing the drug device for colon specific drug delivery, plasma peak is obtained at an optimal time, numbers of doses per day can be reduced, saturated first pass metabolism and tolerance development can also be avoided (10)(11)(12).…”

Section: Introductionmentioning

confidence: 99%

CPVA Grafted Poly(sodium 4-styrene sulfonate) and Studies on its Colon Specific for Chronotherapy of Nocturnal Asthma

Men

Gao

Wang

et al. 2013

Journal of Macromolecular Science, Part A

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The paper attempted to develop a colon specific drug delivery system using CPVA grafted poly (sodium 4-styrene sulfonate)(SSS), namely CPVA-g-PSSS microsphere, loaded with theophylline (TP) for chronotherapy of nocturnal asthma. The grafted CPVA-g-PSSS microspheres were prepared by surface-initiated graft-polymerization, and their surface charges were determined by testing Zeta potential. On this basis, the adsorption property of the grafted microspheres CPVA-g-PSSS for theophylline, namely drug loading ability, was mainly investigated, and the adsorption mechanism was explored. The in vitro release behavior of the drug-loaded microspheres was also examined at different pH value and in simulated gastrointestinal fluids. The experiments show the CPVA-g-PSSS microspheres exhibit strong adsorption ability (38.5 mg/g) for TP by driving of electrostatic interaction in an acidic medium. The in vitro release behavior of the drug-loaded microspheres is highly pH-sensitive. The in vitro release in simulated gastrointestinal (GI) fluid reveals that drug does not release in the stimulated gastric fluid (pH 1), while in the simulated colonic fluid (pH 7.4), a burst release phenomenon occurs, and 52% TP is released in one hour. An excellent colon-specific drug delivery system is developed to realize a lag time of drug release in 6 h runtime of upper gastrointestinal tract, which should be consistent with the demands of chronotherapy of nocturnal asthma.

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“…Moreover, small difference in pH between the small intestine and the colon makes it alone as a less reliable approach [26]. Kadam et al have reported theophylline loaded pellets using the combination of time-dependent and pH-sensitive polymers as Eudragit RL100 and Eudragit S100, respectively to develop more reliable colon targeted system [27].…”

Section: Introductionmentioning

confidence: 99%

Formulation Development of Colon Targeted Mesalamine Pellets: In Vitro-in Vivo Release Study

Bahekar

Wadher

2019

Int J App Pharm

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Objective: This study was intended to investigate the potential of the colon specificity approach comprising of use of pH-sensitive and time-dependent polymers in combination for precise colonic release of Mesalamine or 5-Aminosalicylic acid (5-ASA). Methods: The extrusion and spheronization method, preferably employed in industry for allowing high dose capacity to formulate, was used to prepare drug pellets. The Wurster coating technique used for aqueous coatings of Eudragit NE 40D as an inner coat and Eudragit FS30D as outer coat. The changing pH media used for in vitro release study of optimization batches for both the coating levels. A scanning electron microscope (SEM) was used to evaluate coating thickness and surface morphology. Results: The pharmacokinetic parameters of formulation evaluated by in vivo study in rabbits revealed that the uncoated formulation released the drug too early in the gastrointestinal tract (GIT) with a mean Cmax of 1205.28±0.37 µg/ml at 2 h after administration, whereas desired lag time was achieved in case of coated pellets exhibiting mean Cmax 465.94±0.21 µg/ml and tmax of 8 h. Conclusion: The in vitro and in vivo release study divulge the reliability of approach involving the use of pH sensitivity and time dependency of polymer for drug release in a single formulation for the treatment of colonic diseases. Hence, the present study provides constructive results for colon targeting of 5-ASA pellets with industrially feasible processes.

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Development of colon targeted multiparticulate pulsatile drug delivery system for treating nocturnal asthma

Cited by 29 publications

References 26 publications

Polymeric nanoparticles for colon cancer therapy: overview and perspectives

Polymeric nanoparticles for colon cancer therapy: overview and perspectives

CPVA Grafted Poly(sodium 4-styrene sulfonate) and Studies on its Colon Specific for Chronotherapy of Nocturnal Asthma

Formulation Development of Colon Targeted Mesalamine Pellets: In Vitro-in Vivo Release Study

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