Colon-specific delivery of 5-aminosalicylic acid from chitosan-Ca-alginate microparticles

Mladenovska, Kristina; Raicki, Renata Slavevska; Janevik-Ivanovska, Emilija; Ristoski, Trpe; Pavlova, Maja Jurhar; Kavrakovski, Zoran; Dodov, Marija Glavaš; Goračinova, Katerina

doi:10.1016/j.ijpharm.2007.05.028

Cited by 151 publications

(71 citation statements)

References 50 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…There is evidence in the literature that both polysaccharides, namely calcium alginate and chitosan, are degraded by bacteria in the colon (1,5,(8)(9)(10)(11). The test was developed in phosphate buffer at pH 7.5, simulating the colonic pH of the medium, in the absence and presence of 9.9×10 −2 U/mL β-glucosidase enzymes.…”

Section: Effect Of β-Glucosidase Enzymes Over 5-asa Released From Thementioning

confidence: 99%

“…Chitosan-alginate drug delivery systems have been described for site-specific drug delivery in the colon (1)(2)(3)(4)(5)(6)(7) due to the fact that polysaccharides, calcium alginate, and chitosan are degraded by bacteria in the colon (1,5,(8)(9)(10)(11). It has been shown that the use of bacteria as a trigger mechanism for colonic drug release shows improved specificity over a pH-responsive approach.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

The Effect of Chitosan as Internal or External Coating on the 5-ASA Release from Calcium Alginate Microparticles

et al. 2010

View full text Add to dashboard Cite

Abstract. The effect of chitosan as internal or external coating on the mesalamine (5-ASA) release from calcium alginate microparticles (CaAl) was studied, and a delayed release of 5-ASA system intended for colonic drug delivery was developed. The external chitosan coating was developed by immersion of wetted CaAl in chitosan solution and the internal coating by mixing 5-ASA with chitosan solution and drying before the preparation of CaAl. Both systems were coated with Acryl-EZE ® using combined fluid bed coating and immersion procedure. The results showed that in phosphate medium (pH 7.5), chitosan as 5-ASA coating promotes a quick erosion process accelerating drug release, but chitosan as external coating (CaAlCS) does not increase the T 50 value compared with the microparticles without chitosan (CaAl). Chitosan as internal or external coating was not effective to avoid the quick 5-ASA release in acidic medium (pH 1.2). The presence of β-glucosidase enzymes increases significantly the 5-ASA release for CaAl, while no effect was observed with chitosan as internal or external coating. Fourier transform infrared spectroscopy, thermogravimetric analysis, and X-ray data revealed that 5-ASA did not form a solid solution but was dispersed in the microparticles. The Acryl-EZE ® coating of microparticles was effective because all the formulations showed a low release, less than 15%, of 5-ASA in acid medium at pH 1.2. Significant differences in the percentage of 5-ASA released between formulations were observed in phosphate buffer at pH 6.0. In phosphate buffer at pH 7.2, all the formulations released 100% of 5-ASA.

show abstract

Section: Effect Of β-Glucosidase Enzymes Over 5-asa Released From Thementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

The Effect of Chitosan as Internal or External Coating on the 5-ASA Release from Calcium Alginate Microparticles

et al. 2010

View full text Add to dashboard Cite

show abstract

“…1 A number of analytical methods has been developed for the analysis of mesalamine in pharmaceutical dosage forms and biological matrices. These methods include voltammetry, 2-4 spectrophotometry, 5,6 spectrofluorometry, 7,8 coulometery, 9 and high-performance liquid chromatography (HPLC) combined with UV, [10][11][12] fluorescence, 13,14 mass spectrometry (MS), 15, 16 and electrochemical (EC) 17 detections.…”

Section: Introductionmentioning

confidence: 99%

Determination of mesalamine by spectrofluorometry in human serum after solid-phase extraction with Ni-Al layered double hydroxide as a nanosorbent

Abdolmohammad‐Zadeh¹,

Kohansal²

2012

J. Braz. Chem. Soc.

View full text Add to dashboard Cite

Hidróxido duplo lamelar de níquel-alumínio nanoestruturado foi sintetizado e o potencial do material obtido, foi avaliado como sorvente para extração em fase sólida (SPE), na separação e pré-concentração de quantidades traço de mesalazina (ácido 5-aminossalicílico) usando o método de coluna. O analito retido em Ni-Al LDH foi removido por solução de NaOH e a concentração de 5-ASA eluída foi então determinada espectrometricamente em λ em = 480 nm com excitação em λ ex = 340 nm. Vários parâmetros experimentais afetando a eficiência da extração de mesalazina em Ni-Al (NO 3 -) LDH, tais como pH, quantidade de sorvente, taxa de fluxo da quantidade de amostra, condições de eluição e volume de amostra, foram investigados. Nas condições experimentais ideais, o limite de detecção e o fator de enriquecimento foram 0,04 e 40 µg L −1 , respectivamente. A curva de calibração do sistema de pré-concentração foi linear no intervalo de 0,1-45,0 µg L −1 com um coeficiente de correlação 0,998. O desvio padrão relativo resultante da análise de seis repetições de soluções de 100 mL contendo 1,0 µg L -1 de mesalazina foi 2,05%. O método otimizado foi aplicado com sucesso na determinação de mesalazina em amostras de soro de sangue. Nanostructured nickel-aluminum layered double hydroxide (Ni-Al LDH) was synthesized and the potential of the obtained material, as solid-phase extraction (SPE) sorbent, for separation and pre-concentration of trace amount of mesalamine (5-aminosalicylic acid) was assessed using column method. The retained analyte on Ni-Al LDH was eluted with NaOH solution and the concentration of the elueted 5-ASA was then spectrofluorometrically determined at λ em = 480 nm with excitation at λ ex = 340 nm. Various experimental parameters affecting the extraction efficiency of mesalamine on Ni-Al (NO 3 -) LDH, such as pH, amount of sorbent, sample loading flow rate, elution conditions and sample volume, were investigated. In the optimum experimental conditions, the limit of detection and enrichment factor were 0.04 and 40 µg L −1 , respectively. The calibration graph for the pre-concentration system was linear in the range of 0.1-45.0 µg L −1 with a correlation coefficient of 0.998. The relative standard deviation (RSD) resulting from the analysis of six replicates of 100 mL solutions containing 1.0 µg L -1 mesalamine was 2.05%. The optimized method was successfully applied to the determination of mesalamine in blood serum samples.

show abstract

“…Mesalazine acts topically on the colonic mucosa but when orally administered, it is extensively and rapidly absorbed in the small intestine, leading to little localization of mesalazine in the colon and hence, low efficiency with significant systemic side effects (2). Consequently, three methods have been commonly used for targeting of mesalazine to the colon: a pro-drug concept, enteric coating, and/or prolonged release of the drug through semipermeable membrane (3).…”

Section: Introductionmentioning

confidence: 99%

Once Daily, High-Dose Mesalazine Controlled-Release Tablet for Colonic Delivery: Optimization of Formulation Variables Using Box–Behnken Design

2011

View full text Add to dashboard Cite

Abstract. The aim of this work was to statistically optimize a novel high-dose, mesalazine colonic delivery matrix system, potentially suitable for once daily administration, using simple wet granulation method. A hydrophobic-hydrophilic polymeric blend was used to manipulate drug release. A three-factor, three-level Box-Behnken design was used to construct polynomial models correlating the dependent and independent variables. Independent formulation variables were the percentages of the hydrophilic polymer Carbopol® 940, hydrophobic polymer Eudragit® RS, and the superdisintegrant croscarmellose sodium. The cumulative percentages of drug released at 6, 10, and 14 h were selected as dependent variables and restricted to 7.5-22.5% (Y 1 ), 42.5-57.5 % (Y 2 ), and 72.5-87.5% (Y 3 ), respectively. A second-order polynomial equation fitted to the data was used to optimize the independent formulation variables. Based on Box-Behnken experimental design, different mesalazine release profiles were obtained. The optimized formulation containing 5.72% Carbopol®, 9.77% Eudragit® RS, and 1.45% croscarmellose sodium was prepared according to the software determined levels. It provided a release profile which was very close to the targeted release profile, where the calculated values of f 1 and f 2 were 8.47 and 67.70, respectively, and followed zero-order release kinetics.

show abstract

Colon-specific delivery of 5-aminosalicylic acid from chitosan-Ca-alginate microparticles

Cited by 151 publications

References 50 publications

The Effect of Chitosan as Internal or External Coating on the 5-ASA Release from Calcium Alginate Microparticles

The Effect of Chitosan as Internal or External Coating on the 5-ASA Release from Calcium Alginate Microparticles

Determination of mesalamine by spectrofluorometry in human serum after solid-phase extraction with Ni-Al layered double hydroxide as a nanosorbent

Once Daily, High-Dose Mesalazine Controlled-Release Tablet for Colonic Delivery: Optimization of Formulation Variables Using Box–Behnken Design

Contact Info

Product

Resources

About