Chitosan coated Ca–alginate microparticles loaded with budesonide for delivery to the inflamed colonic mucosa

Crcarevska, Maja Simonoska

doi:10.1016/j.ejpb.2007.06.007

Cited by 134 publications

(55 citation statements)

References 42 publications

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“…The thermograms of both empty ( Figure 3D) and PG-loaded MPs ( Figure 3E) show disappearance of the degradation exothermic peaks of chitosan at 310 C and of pectin at 240 C, as well as pectin endothermic peaks which could be attributed to the electrostatic interactions between pectin and chitosan. Similar results were previously reported for chitosan-alginate polyelectrolyte complex (Simonoska Crcarevska et al, 2008). The thermogram of PG-loaded MPs ( Figure 3E) shows the characteristic melting peak of PG with no change in the peak shape or position confirming the absence of physical or chemical interactions with the microparticle components.…”

Section: Differential Scanning Calorimetry Studiessupporting

confidence: 76%

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

et al. 2015

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The colon is a promising target for drug delivery owing to its long transit time of up to 78 h, which is likely to increase the time available for drug absorption. Progesterone has a short elimination half-life and undergoes extensive first-pass metabolism, which results in very low oral bioavailability ($25%). To overcome these shortcomings, we developed an oral multiparticulate system for the colonic delivery of progesterone. Zn-pectinate/chitosan microparticles were prepared by ionotropic gelation and characterized for their size, shape, weight, drug entrapment efficiency, mucoadhesion and swelling behavior. The effect of crosslinking pH, cross-linking time and chitosan concentration on progesterone release were also studied. Spherical microparticles having a diameter of 580-720 mm were obtained. Drug entrapment efficiency of $75-100% was obtained depending on the microparticle composition. Microparticle mucoadhesive properties were dependent on the pectin concentration, as well as the cross-linking pH. Progesterone release in simulated gastric fluids was minimal (3-9%), followed by burst release at pH 6.8 and a sustained phase at pH 7.4. The in vivo study revealed that the microparticles significantly increased progesterone residence time in the plasma and increased its relative bioavailability to $168%, compared to the drug alone. This study confirms the potential of Zn-pectinate/chitosan microparticles as a colon-specific drug delivery system able to enhance the oral bioavailability of progesterone or similar drugs.

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Section: Differential Scanning Calorimetry Studiessupporting

confidence: 76%

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

et al. 2015

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“…This suggests formation of flocculated and stable suspensions in aqueous medium, which, in turn, build up noncompacted aggregates that are easy to resuspend by the time they settle. 46 …”

Section: Encapsulation Efficiency For Methylprednisolonementioning

confidence: 99%

Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique

Tobar-Grande¹,

Godoy²,

Bustos³

et al. 2013

IJN

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Abstract:In this work, microparticles were prepared by spray-drying using albumin, chondroitin sulfate, and hyaluronic acid as excipients to create a controlled-release methylprednisolone system for use in inflammatory disorders such as arthritis. Scanning electron microscopy demonstrated that these microparticles were almost spherical, with development of surface wrinkling as the methylprednisolone load in the formulation was increased. The methylprednisolone load also had a direct influence on the mean diameter and zeta potential of the microparticles. Interactions between formulation excipients and the active drug were evaluated by x-ray diffraction, differential scanning calorimetry, and thermal gravimetric analysis, showing limited amounts of methylprednisolone in a crystalline state in the loaded microparticles. The encapsulation efficiency of methylprednisolone was approximately 89% in all formulations. The rate of methylprednisolone release from the microparticles depended on the initial drug load in the formulation. In vitro cytotoxic evaluation using THP-1 cells showed that none of the formulations prepared triggered an inflammatory response on release of interleukin-1β, nor did they affect cellular viability, except for the 9.1% methylprednisolone formulation, which was the maximum test concentration used. The microparticles developed in this study have characteristics amenable to a therapeutic role in inflammatory pathology, such as arthritis.

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“…Chitosan and its derivatives have been widely used in biomedical engineering and formulation of drug delivery systems (15). Chitosan has been formulated into microspheres, tablets, and membranes (16,17) as drug delivery carriers. As chitosan can form films easily, it was used to coat the microspheres including poly(lactic acid)-poly(caprolactone) blend.…”

Section: Introductionmentioning

confidence: 99%

Chitosan-Modified PLGA Nanoparticles with Versatile Surface for Improved Drug Delivery

2013

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Abstract. Shortage of functional groups on surface of poly(lactide-co-glycolide) (PLGA)-based drug delivery carriers always hampers its wide applications such as passive targeting and conjugation with targeting molecules. In this research, PLGA nanoparticles were modified with chitosan through physical adsorption and chemical binding methods. The surface charges were regulated by altering pH value in chitosan solutions. After the introduction of chitosan, zeta potential of the PLGA nanoparticle surface changed from negative charge to positive one, making the drug carriers more affinity to cancer cells. Functional groups were compared between PLGA nanoparticles and chitosan-modified PLGA nanoparticles. Amine groups were exhibited on PLGA nanoparticle surface after the chitosan modification as confirmed by Fourier transform infrared spectroscopy and X-ray photoelectron spectroscopy. The modified nanoparticles showed an initial burst release followed by a moderate and sustained release profile. Higher percentage of drugs from cumulative release can be achieved in the same prolonged time range. Therefore, PLGA nanoparticles modified by chitosan showed versatility of surface and a possible improvement in the efficacy of current PLGA-based drug delivery system.

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Chitosan coated Ca–alginate microparticles loaded with budesonide for delivery to the inflamed colonic mucosa

Cited by 134 publications

References 42 publications

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique

Chitosan-Modified PLGA Nanoparticles with Versatile Surface for Improved Drug Delivery

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