Chitosan–pectin multiparticulate systems associated with enteric polymers for colonic drug delivery

Oliveira, Giselle F.; Ferrari, Priscileila Colerato; Carvalho, Livia Q.; Evangelista, Raul Cesar

doi:10.1016/j.carbpol.2010.06.041

Cited by 81 publications

(26 citation statements)

References 27 publications

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“…Figure 5 shows that the MPs had a moderate swelling in SGF during the first 15 min where the swelling index was $150% and remained at that level for the rest of the study period. At the low pH of SGF, the carboxyl groups of pectin were not ionized, which reduced the repulsive forces among the polymer chains and decreased their swelling (Oliveira et al, 2010). Although chitosan was fully ionized in SGF and could increase the MP swelling, its lower concentration (0.5%) compared to that of pectin (4%) limited its effect on the MP swelling.…”

Section: Microparticle Swelling Behaviormentioning

confidence: 96%

“…Pectin is non-toxic and not affected by gastric or intestinal enzymes while being completely degraded by pectinolytic enzymes produced by microflora in the colon (Bourgeois et al, 2006). The amidated low methoxy (LM) pectin, in which some of the carboxylic acid groups are amidated, is more tolerant to pH variations which makes it an appropriate candidate for the design of colon-targeted drug delivery systems (Oliveira et al, 2010). However, pectin high aqueous solubility and swelling properties are considered the major drawbacks that lead to rapid drug release during transit in the upper GIT (Maestrelli et al, 2008a;Wei et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

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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: Microparticle Swelling Behaviormentioning

confidence: 96%

Section: Introductionmentioning

confidence: 99%

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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“…SD 1:10:10 and SD 1:15:15 exhibited low drug release rates in acid media releasing 19% (± 0.0012) and 37% (± 0.0184) of drug, respectively in 30 min. This behavior can be attributed to the gastro-resistance properties of HPMCP, which exhibited lower swelling in this medium (Table 1), avoiding erosion and contributing to decreasing drug release rates (Oliveira et al, 2010). Indeed, it can be observed despite the presence of HPMCP, an enteric polymer, the drug release rates in the first 15 minutes were very similar for both acid and enteric media.…”

Section: Resultsmentioning

confidence: 72%

“…Increased liquid uptake values in the simulated enteric medium indicated that increases in pH should favor carboxyl group repulsion in HPMCP, causing the chains to move farther apart loosening the polymer matrix. Both of these factors favor the entrance of water molecules (Oliveira et al, 2010).…”

Section: Resultsmentioning

confidence: 99%

A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability

Pedreiro

Cury

Chaud

et al. 2016

Braz. J. Pharm. Sci.

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Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this property significantly increased with higher pH values. SDs allowed drug dissolution to occur in a controlled manner. HPMCP decreased the dissolution rates in the acid medium. The mucoadhesiveness of SDs was demonstrated and the permeability of AZT carried in solid dispersions was significantly improved. The effect of the SD carrier polymers on blocking efflux pump can be an important approach to improve the bioavailability of AZT.Uniterms: Zidovudine. Solid dispersion. Mucoadhesion. P-glycoprotein. Intestinal permeability.

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“…The addition of CAP and HPMCP resulted in the highest control over the drug release in all media. CAP-Triamcinolone formulation presented the slowest drug release rate, of only 1.33%, in acidic medium after 2h, while the control formulation released 45.52% after the same time 58 . Nanoparticulate colloidal carriers composed of natural or synthetic polymers have also been investigated for colon targeting 59 .…”

Section: 2mentioning

confidence: 91%

Multiparticulate Combined Approaches for Colon Specific Drug Delivery

Pradhan¹

2011

Int Jour of Biomed Res

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In order to achieve a successful colon targeted drug delivery system, a drug needs to be protected from degradation, release and/or absorption in the upper portion of the gastrointestinal tract (GIT) and then ensure abrupt or controlled release in the proximal colon. Such a system can be formulated by utilizing microbial triggering degradation of polymer coating/ gastro intestinal (GI) transit time (time dependent)/ pH dependent approach etc. But unfortunately it has been found that colonic microflora, GI transit time and pH varies considerably inside a human system by several factors, in addition to this the native biodegradable polysaccharides which are used widely for the microbial triggering colonic drug delivery system (CDDS), are having high aqueous solubility on account of which a single unit colon targeted drug delivery systems may suffer from dose dumping due to overall catastrophic failure of the film around a monolith, which would then release the whole drug, that may lead to drastically compromised systemic drug bioavailability or loss of local therapeutic action in the colon. This review emphasizes some of the causes which make a single unit dosage form unsuitable for targeting to colon by using microbial triggering/GI transit time/pH dependent approach, and at the same time discusses researches which have been carried out to alleviate these problems by utilizing multiparticulate combined approaches.

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Chitosan–pectin multiparticulate systems associated with enteric polymers for colonic drug delivery

Cited by 81 publications

References 27 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

A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability

Multiparticulate Combined Approaches for Colon Specific Drug Delivery

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