Biopelículas activas de extracto acuosos de Gliricidia sepium y su influencia en la vida útil microbiológica del queso costeño / Active biofilms of aqueous extract of Gliricidia sepium and its influence on the microbiological shelf life of coastal cheese

RESUMEN La elaboración de biopelículas con propiedades bioactivas es un área interesante en el campo de los empaques alimentarios. El objetivo de este estudio fue obtener biopelículas activas (BPA) a base de extracto acuoso de hojas de Gliricidia sepium y determinar su efecto en la vida útil microbiológica del queso costeño. Para la fabricación de las BPA, el extracto acuoso fue microencapsulado, mediante gelación iónica y, posteriormente, incorporado en las biopelículas. La determinación de la vida útil de muestras de queso costeño, se llevó a cabo mediante microbiología predictiva, utilizando el modelo de Monod Hinshelwood. Las microcápsulas utilizadas tuvieron un diámetro promedio de 273,786µm. Los resultados mostraron un aumento en la vida útil microbiológica de 26,7 días, en quesos con BPA, almacenado a 7°C, en comparación con una muestra control (sin BPA), confirmando que las BPA investigadas ejercen un efecto inhibitorio sobre los microorganismos, causantes de deterioro en quesos. Por tal motivo, la metodología aquí planteada puede ser una alternativa en la conservación de un producto perecedero, como el queso costeño.

ABSTRACT The elaboration of biofilms with bioactive properties is an interesting area in the field of food packaging. The aim of this study was to obtain active biofilms (AB) based on aqueous extract of Gliricidia sepium leaves and determine their effect on the microbiological shelf life of coastal cheese. For the manufacture of the AB, the aqueous extract was microencapsulated by means of ionic gelation and later incorporated in the biofilms. The coastal cheese's shelf life was carried out by means of predictive microbiology using the Monod Hinshelwood model. The microcapsules had an average diameter of 273.786µm. The results showed an increase in the microbiological shelf life of 26.7 days in cheeses with AB stored at 7°C compared with control sample (without AB) confirming that the AB investigated exerts an inhibitory effect on the microorganisms causing deterioration in cheeses. For this reason, the methodology proposed here can be an alternative in the conservation of a perishable product such as coastal cheese.

Bioactive compounds in jamelão yogurt (Syzygium cumini L) / Compostos bioativos em iogurte de jamelão (Syzygium cumini L)

The jamelão fruit has been used in traditional Indian medicine and has recently attracted interest as a functional food, as it is rich in anthocyanins. Anthocyanins are of interest of the food industry due to their antioxidant power, attractive color and stability in acid-rich foods. This research used the gelation process with sodium alginate solution to obtain bioactive yogurt from the production of jamelão capsules added to natural yogurt. The proportion was 80% yogurt and 20% jellybean pulp capsules. The treatments were control yogurt (without the addition of jamelão capsules), jamelão capsules and bioactive yogurt (with the capsules). The objective was to study the antioxidant activity, physical-chemical, nutritional and microscopic stability of the product kept under refrigeration for 28 days at 4±1ºC. The addition of jamelão capsules in the yogurt changed the product's physical properties (increased humidity and decreased Brix and ash). There was an increase in the amount of phenols and anthocyanins, in addition to the antioxidant potential at 28 days of storage. The interior of the microcapsules was composed of a mesh structure through which the encapsulated material was distributed, as the capsules can be added to yogurt, to improve the antioxidant and nutritional capacity, which proves to be a promising and viable alternative.

A fruta Jamelão tem sido usada na medicina tradicional indiana e recentemente atrai interesse como alimento funcional, por ser rica em antocianinas. As antocianinas são de interesse da indústria de alimentos devido ao seu poder antioxidante, cor atraente e estabilidade em alimentos ácidos. Esta pesquisa utilizou o processo de gelificação com solução de alginato de sódio para obter iogurte bioativo, a partir da produção de cápsulas de jamelão adicionadas em iogurte natural. A proporção utilizada foi de 80% de iogurte e 20% de cápsulas de polpa de jamelão. Os tratamentos foram iogurte controle (sem adição de cápsulas de jamelão), cápsulas de jamelão e iogurte bioativo (contendo as cápsulas). O objetivo foi estudar a atividade antioxidante, a estabilidade físico-química, nutricional e microscópica do produto mantido sob refrigeração por 28 dias a 4 ± 1 ºC. A adição de cápsulas de jamelão no iogurte alterou as propriedades físicas do produto (aumento de umidade, diminuição de Brix e cinzas). Houve aumento na quantidade de fenóis e antocianinas, além do potencial antioxidante aos 28 dias de armazenamento. O interior das cápsulas era composto por uma estrutura em malha através da qual o material encapsulado foi distribuído. Desta forma, as cápsulas podem ser um ingrediente adicionado ao iogurte, melhorando a capacidade antioxidante e nutricional, provando ser uma alternativa promissora e viável.

Evaluación de la estabilidad de cápsulas de jugo de naranja obtenidas mediante gelificación iónica / Evaluation of the stability of orange juice capsules obtained by ionic gelation

Resumen El método de gelificación iónica, como técnica de encapsulación, se basa en las interacciones entre hidrocoloides, las cuales previenen la posibilidad de daño de compuestos bioactivos presentes en alimentos, tales como los jugos de cítricos. El objetivo del presente estudio fue evaluar la estabilidad de las cápsulas de jugo de naranja, obtenidas mediante gelificación iónica, utilizando pectina y alginato de sodio como agentes encapsulantes. Se determinaron la pérdida de peso, atributos de color, diámetro, morfología macroscópica y densidad en cápsulas elaboradas. Se utilizó un diseño factorial, modificando la concentración de pectina de alto metoxilo (1.5 %, 2 % y 2.5 % p/v), pH (2.5, 3.5 y 4.5) y sólidos solubles totales (SST) a 5 ºBrix y 15 ºBrix, manteniendo constante la concentración de alginato de sodio al 0.5 % (p/v), y se almacenaron a temperatura ambiente (26 ºC) y refrigeración (4 ºC) durante 12 d. Las cápsulas presentaron principalmente forma esférica (> 45 %). Los atributos de color permanecieron estables durante 12 d de almacenamiento. Los SST iniciales y el pH influyeron en la estabilidad de las cápsulas. A una concentración de 15 ºBrix y pH 2.5 no se pudieron formar de manera adecuada las cápsulas, presentando mayor sinéresis y morfologías amorfas. Las cápsulas de jugo de naranja con concentración de pectina 2 % (p/v), alginato de sodio 0.5 % (p/v), SST 5 ºBrix y pH 2.5, se mantuvieron estables con parámetros de calidad apropiados al ser almacenadas a temperatura de refrigeración (4 ºC). El método de gelificación iónica mediante encapsulación ofrece una alternativa para prolongar la vida útil del jugo, y el desarrollo de nuevos productos elaborados a partir de este cítrico.

Abstract The ionic gelation method as an encapsulation technique is based on the interactions between hydrocolloids, which prevent the possibility of damage of bioactive compounds present in foods, such as citrus juice. Therefore, the objective of the present study was to evaluate the stability of the orange juice capsules obtained by ionic gelation using pectin and sodium alginate as encapsulating agents. The effects of the gelling agents on the stability were determined by the measurement of weight loss, diameter, color attributes, diameter, macroscopic morphology, density in elaborate capsules. In addition, a factor analysis design was used by modifying the concentration of high methoxyl pectin (1.5 %, 2 % and 2.5 % w/v), pH (2.5, 3.5 and 4.5) and total soluble solids (TSS) at 5 ºBrix and 15 ºBrix, maintaining the concentration of sodium alginate constant at 0.5 % (w/v). The capsules were stored at room temperature (26 ºC) and refrigeration (4 ºC) for 12 d. They mainly presented a spherical shape (> 45 %). The color attributes remained stable even after 12 d of storage. The initial TSS and pH influenced the stability of the capsules. At a concentration of 15 ºBrix and pH 2.5, the capsules could not be adequately formed, capsules presenting greater syneresis and amorphous morphologies. However, the orange juice capsules remained stable for more than 2 weeks and with stable quality parameters when stored at refrigeration temperature (4 ºC), pectin concentration 2 % (w/v), sodium alginate 0.5 % (w/v), TTS 15 ºBrix and pH 2.5. The ionic gelation method through encapsulation offers an alternative to extend the shelf life of the juice and the development of new products made from this citrus.

Improvement of the viability of probiotics (Lactobacillus acidophilus) by multilayer encapsulation / Melhoramento da viabilidade de probióticos (Lactobacillus acidophilus) por encapsulação em multicamadas

ABSTRACT: This study produced pectin microcapsules containing Lactobacillus acidophilus by external ionic gelation, followed by the adsorption of whey protein and pectin to form multilayers. The viability of free and microencapsulated lactobacilli was evaluated after in vitro exposure to gastrointestinal conditions. They were also assessed by heat treatment, and stability was examined at -18 °C, 5 °C and 25 °C for 120 days. Exposure to different pHs, simulating passage through the gastrointestinal tract, showed that treatment of the microcapsules with only pectin (LA/P0) and with one and two layers of whey protein (treatments LA/P1 and LA/P3, respectively), were able to protect Lactobacillus acidophilus , with microcapsules increasing the release of probiotics from the stomach into the intestines. Free cells showed a decrease in their counts over the course of the simulated gastrointestinal system. Regarding heat treatments, microcapsules with a layer of whey protein (LA/P1) maintained the viability of their encapsulated Lactobacillus acidophilus (9.57 log CFU/g-1). The best storage viability was at -18 °C, with a count of 7.86 log CFU/g-1at 120 days for microcapsule LA/P1,with those consisting of two layers of whey protein (LA/P3)having a 6.55 log CFU/g-1 at 105 days. This study indicated that external ionic gelation was effective and could be used for the production of pectin microcapsules, with multilayer whey protein promoting greater protection and viability of Lactobacillus acidophilus.

RESUMO: O objetivo deste trabalho foi produzir microcápsulas de pectina, contendo Lactobacillus acidophilus por gelificação iônica externa, seguida da adsorção de proteína de soro de leite e multicamadas formadoras de pectina. Além disso, a viabilidade de lactobacilos livres e microencapsulados, após exposição in vitro a condições gastrintestinais, foi avaliada após simulação de tratamentos térmicos e, finalmente, estabilidade a -18 ºC, 5 ºC e 25 ºC durante 120 dias de armazenamento. A exposição a diferentes pHs, simulando a passagem pelo trato gastrointestinal, mostrou que os tratamentos das microcápsulas com apenas pectina (LA/P0) e com uma e duas camadas proteína do soro (tratamentos LA/P1 e LA/P3, respectivamente), foram capazes de proteger o Lactobacillus acidophilus , enquanto as microcápsulas aumentaram a liberação de probióticos do estômago para o intestino. As células livres diminuíram suas contagens no curso do sistema. Em relação aos tratamentos térmicos aplicados, pode-se afirmar que a microcápsula com uma camada de proteína do soro (LA/P1) resistiu e manteve a viabilidade de Lactobacillus acidophilus (9,57 log CFU / g-1). A melhor viabilidade foi obtida no armazenamento a -18 ° C, com uma contagem de 7,86 log CFU / g-1 para essa mesma microcápsula (LA/P1) no final do armazenamento (120 dias) e 6,55 log CFU / g-1 para as microcápsulas com duas camadas de proteína do soro (LA/P3) por 105 dias. Este estudo indica que a gelificação iônica externa é eficaz e pode ser usada para a produção de microcápsulas de pectina com multicamadas de proteína de soro para promover maior proteção e viabilidade ao Lactobacillus acidophilus.

Production and characterization of alginate microparticles obtained by ionic gelation and electrostatic adsorption of concentrated soy protein / Produção e caracterização de micropartículas de alginato obtidas por gelificação iônica e adsorção eletrostática de concentrado proteico de soja

ABSTRACT: Microencapsulation is used for protection and release of bioactive compounds. Combination of encapsulation methods allows the production of matrices with better technological properties compared to the application of one of the methods alone. Use of ionic gelation produces porous microparticles, and coating it with a protein, by electrostatic interaction, may contribute to a better protection of the active compound. The objective of the research was to produce alginate microparticles (AG) through ionic gelation and to coat them with soluble protein from soy protein concentrate. Two factors were studied, calcium concentration during ionic gelation (0.8, 1.6 and 2.4% w/w) and pH (3.5 and 7.0) of the protein solution for electrostatic interaction. Zeta potential (ZP) of biopolymers and microparticles were determined. Microparticles were characterized according to its morphology, average size and size distribution, as well as protein adsorption. Microparticles presented (154-334μm) multinuclear distribution of active compound, continuous and smooth surface, with a great standard deviation considering average size. The calcium concentration did not influence the protein adsorption on microparticles.The pH used in protein adsorption showed significant effect, with higher adsorption occurring at pH 3.5 (6.5 to 6.7% w/w, dry basis,db, of adsorbed protein) compared to pH 7.0 (<2.0% w/w, db, of adsorbed protein) indicating that electrostatic interaction was determinant for the protein coating. At this situation, ionic gelation microparticles and proteins presented ZP with opposite charges (pH>pKa AG<Isoelectric point, IP).

RESUMO: A microencapsulação é utilizada para a proteção de compostos bioativos e controle de sua liberação. A combinação de métodos de encapsulação permite a obtenção de matrizes com melhores propriedades tecnológicas em relação às técnicas utilizadas individualmente. Na gelificação iônica são produzidas micropartículas porosas, e o recobrimento por interação eletrostática com uma proteína permite a obtenção de micropartículas mais protetivas. O objetivo do trabalho foi produzir micropartículas de alginato (AG) através da gelificação iônica e recobri-las com proteínas solúveis de concentrado proteico de soja. Dois fatores foram estudados, o teor de cálcio utilizado na gelificação iônica (0,8,1,6 e 2,4% m/m) e o pH (3,5 e 7,0) para o recobrimento eletrostático com uma camada proteica. Os potenciais zeta (PZ) dos biopolímeros e das micropartículas foram determinados. As micropartículas foram caracterizadas quanto a morfologia, tamanho médio e sua distribuição e quanto ao teor de proteína adsorvida nas situações estudadas. As micropartículas obtidas apresentaram-se (154-334μm) com recheio distribuído de forma multinuclear, com superfície continua e visualmente lisas, porém com variação grande no tamanho médio. A variação do teor de cálcio não foi significativa na adsorção proteica. O pH utilizado na adsorção proteica foi significativo, com adsorções muito maiores em pH 3,5 (6,5 - 6,7% m/m de proteína adsorvida, base seca) comparado ao pH 7,0 (<2,0% m/m de adsorção proteica, base seca), indicando que a interação eletrostática foi determinante no recobrimento proteico. Nesta situação, micropartículas AG e a proteína apresentam PZ com cargas opostas (pH>pKa AG<ponto isoeletrico, PI).

Comparative Study of Poly(L-Lactic Acid) Scaffolds Coated with Chitosan Nanoparticles Prepared via Ultrasonication and Ionic Gelation Techniques

In this study, an attempt was made to develop bi-functional constructs serving both as scaffolds and potential delivery systems for application in neural tissue engineering. The constructs were prepared in two steps. In the first step, the bulks of poly (L-lactic acid) (PLLA) in 1, 4-dioxane/water (87:13) were fabricated using liquid-liquid thermally induced phase separation technique. In the next step, the prepared bulks were coated with chitosan nanoparticles produced by two different techniques of ultrasonication and ionic gelation by grafting-coating technique. In ultrasonication technique, the chitosan solution (2 mg/mL) in acetic acid/sodium acetate buffer (90:10) was irradiated by an ultrasound generator at 20 kHz and power output of 750 W for 100 s. In ionic gelation technique, the tripolyphosphate in water solution (1 mg/mL) was added to the same chitosan solution. The physicochemical properties of the products were characterized by Scanning Electron Microscopy, Attenuated Total Reflection Fourier Transform-Infrared, liquid displacement technique, contact angle measurement, compressive and tensile tests, as well as zeta potential and particle size analysis using dynamic light scattering. Moreover, the cell proliferation and attachment on the scaffolds were evaluated through human glioblastoma cell line (U-87 MG) and human neuroblastoma cell line [BE (2)-C] culture respectively. The results showed that the samples coated with chitosan nanoparticles prepared by ultrasonication possessed enhanced hydrophilicity, biodegradation and cytocompatibility compared with pure PLLA and PLLA coated with chitosan nanoparticles prepared by ionic gelation. This study suggests successful nanoparticles-scaffold systems which can act simultaneously as potential delivery systems and tissue engineering scaffolds.

Preparation,formulation optimization and preliminary pharmacodynamic experi-ment of insulin-loaded N-trimethyl chitosan nanoparticles / 药学实践杂志

Objective To prepare and optimize insulin-loaded N-trimethyl chitosan nanoparticles via orthogonal design , and preliminarily study the effects on blood glucose level .Methods The insulin-loaded N-trimethyl chitosan nanoparticles (INS-NPs) were prepared by ionic gelation ,and the optimal proportion was obtained with orthogonal design .The nanoparticles were characterized by transmission electron microscopy and zeta/sizer nano analyzer .The entrapment efficiency of insulin-load-ed nanoparticles and the in vitro releasing characteristics were studied by HPLC .A preliminary pharmacodynamic study of the insulin-loaded nanoparticles was also carried out .Results The INS-NPs exhibited narrow distribution .The mean diameter of INS-NPs was (63 .26 ± 1 .88)nm ,while the entrapment efficiency was (37 .92 ± 2 .11)% .After 8 hours of subcutaneous injec-tion of the INS-NPs ,the blood glucose level in diabetic rats decreased to normal level and kept stable .Conclusion The opti-mized insulin-loaded nanoparticles had homogeneous spherical shape ,small size ,and could be a new approach of administration for insulin .

Design and Evaluation of Imatinib Mesylate Loaded Microspheres for Stomach Specific Drug Delivery.

Aims: The aim of the present work was to design and evaluate the Imatinib mesylate microspheres using natural and semi synthetic polymers for stomach specific drug delivery. Study Design: Design and Evaluation of Imatinib Mesylate loaded microspheres Place and Duration of the Study: The study was carried out in Department of Pharmaceutics, JKKMMRF’s Annai JKK Sampoorani Ammal College of Pharmacy, between November 2012 and July 2013. Methodology: The microspheres were prepared using Sodium alginate as a polymer by Emulsification Ionic Gelation Technique. Copolymers of natural origin namely Guar gum, Karaya gum, Chitosan and semi synthetic origin namely Hydroxy propoylmethyl cellulose K4M, K15M, K100M are used as mucoadhesive polymers. The prepared microspheres were evaluated for their percentage yield, entrapment efficiency, degree of swelling, particle size, surface morphology and in-vitro mucoadhesion, drug release studies. Drug release kinetics was determined from drug release data. Selected formulations are subjected to stability studies under varying conditions of temperature and humidity. Results: The production yields of microspheres were found to be between 76.74 to 88.18%. Percentage drug entrapment efficiency of Imatinib mesylate microspheres was ranged from 65.51 to 88.78%. Particle size of the prepared microspheres was in the size range of 440-810μm. SEM analysis revealed that all the prepared microspheres were discrete, spherical in shape. The in-vitro mucoadhesive study demonstrated that Hydroxy propoylmethyl cellulose adhered to the mucus to a greater extent than other polymers. The in-vitro release study shows that, retarded release with increase in percentage of polymers. The release of drug from the microspheres followed Krosmeyer Peppas kinetics. After the stability studies, the formulations remained stable at the end of storage period. Conclusion: Based on the results, it was concluded that, the formulations with natural polymers were found to be best than semi synthetic polymers for the oral delivery of Imatinib mesylate.

Development of natural gum based glipizide mucoadhesive microsphere.

The objective of this study was to develop glipizide microsphere with natural gums. Guar gum and xanthan gum were used separately in different ratios as natural polymers. The microspheres were prepared by orifice ionic gelation method and they were characterized by scanning electron microscopy and particle size analysis. Among six formulations, microspheres of four formulations (F1-F4) were discrete, sphrerical and free flowing. There was an inverse relationship found between the amount of gum and surface smoothness in case of guar gum-containing microspheres while a forward relationship was found between amount of gum and surface smoothness in case of the microspheres containing xanthan gum. The size of the particles increased with increasing amounts of gum. It can be concluded that guar gum and natural gum at a ratio of 1:0.25 and 1:0.5 can be ideal for formulating natural gum based glipizide mucoadhesive microsphere.

Obtención de microcápsulas de tamaño controlado conteniendo Lactococcus lactis, utilizando mezclas de gelanos de alto y bajo acilo / Obtaining size-controlled microcapsules by ionic gelation with high and low acyl gellans containing Lactococcus lactis

Control the diameter of microcapsules obtained with functional biopolymer is a crucial parameter in the success of food applications, since it affects the protection of microencapsulated microorganism and also in the texture of the final product. The aim of this study was to assess the obtaining of controlled size microcapsules containing Lactococcus lactis, using mixtures of high acyl gellan (HA) and low acyl gellan (LA). A concentration of 0.2% (w/w) gellan was employed using a simple design, generating the following mixtures: 100HA/0.0LA, 0.0HA/100LA, 25HA/75LA, 50HA/50LA and 75HA/25LA. The diameter of the microcapsules, efficiency of microencapsulation and viability of the microencapsulated microorganism were studied in function of the speed of agitation (400-800 rpm) and surfactant concentration (sorbitan monooleate) (0.0-0.2%)v/v. The results indicated that mixtures with concentration equal or greater than 50% of HA gellan are not efficient for obtaining microcapsules, only the LA gellan and the mixture 25HA/75LA gave acceptable results. The viability of the microorganism and the efficiency of microencapsulation were descending function of the stirring speed and surfactant concentration. The microcapsules obtained had diameters not greater than 80 µm when the highest concentrations of surfactant (0.2% v/v) and stirring speed (800 rpm) were used, suggesting that the ionic gelation can be used to obtain microcapsules of controlled size (15-75 µm) containing Lactococcus lactis with high viability (83.32%) and high efficiency of microencapsulation (82.4%), which makes it feasible for use in food applications.

Controlar el diámetro de microcápsulas obtenidas con biopolímeros funcionales es un parámetro crucial en el éxito de aplicaciones alimentarias, ya que influye en la protección del microorganismo microencapsulado y también en la textura del producto final. El objetivo de este trabajo fue evaluar la obtención de microcápsulas de tamaño controlado conteniendo Lactococcus lactis, utilizando mezclas de gelana de alto (HA) y bajo acilo (LA). Se empleó una concentración de gelana de 0.2% p/p usando un diseño de mezclas simple, generando las siguientes mezclas, 100HA/0.0LA, 0.0HA/100LA, 25HA/75LA, 50HA/50LA, 75HA/25LA. El diámetro de las microcápsulas, la eficiencia de microencapsulación y la viabilidad del microorganismo microencapsulado fueron estudiadas en función de la velocidad de agitación (400-800 rpm) y concentración de surfactante (sorbitan monooleate) (0.0-0.2%)v/v. Los resultaron indicaron que las mezclas con concentración igual o superior al 50% de gelana de HA, no son eficientes para obtener microcápsulas; solamente dieron resultados aceptables la gelana de LA y la mezcla 25HA/75LA. La viabilidad del microorganismo y la eficiencia de microencapsulación variaron en función descendente de la velocidad de agitación y concentración de surfactante. Las microcápsulas obtenidas no presentaron diámetros superiores a 80 µm cuando se emplearon las mayores concentraciones de surfactante (0.2%) y velocidad de agitación (800 rpm), sugiriendo que la gelación iónica puede ser utilizada para obtener microcápsulas de tamaño controlado (15-75 µm) conteniendo Lactococcus lactis con alta viabilidad (83.32%) y eficiencia de microencapsulación (82.4%), cuando se utiliza la mezcla 25HA/75LA a 800 rpm y 0.2% v/v de surfactante, lo cual la hace factible para su uso en aplicaciones alimentarias.

Colon specific drug delivery of mesalamine using eudragit S100-coated chitosan microspheres for the treatment of ulcerative colitis.

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72%-82.27%, drug loading from 20.28%-33.26%. The size of the prepared microspheres ranged between 61.22-90.41μm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. Micromeritic properties showed good flow properties and packability of prepared microspheres. The drug release of mesalamine from microspheres was found to decrease as the polymer concentration increases. The release profile of mesalamine from eudragit-coated chitosan micro-spheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.

Colon specific drug delivery of mesalamine using eudragit S100-coated chitosan microspheres for the treatment of ulcerative colitis.

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72%-82.27%, drug loading from 20.28%-33.26%. The size of the prepared microspheres ranged between 61.22-90.41μm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. Micromeritic properties showed good flow properties and packability of prepared microspheres. The drug release of mesalamine from microspheres was found to decrease as the polymer concentration increases. The release profile of mesalamine from eudragit-coated chitosan micro-spheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.

Experimental study on surface modification of intraocular lens by cyclosporine A-loaded chitosan nanoparticle / 中华实验眼科杂志

Background Posterior capsular opacification (PCO) following cataract extracapsular extraction is a major cause of the reduction of visual acuity.Topical administration of eye drops is a research hotspot for the prevention of PCO.Objective This study was to evaluate the release of cyclosporine A-loaded chitosan nanoparticles (CyA-CS-NP) by ionic gelation in vitro and its feasibility of modification of the surface of polymethylmethacrylate intraocular lens (PMMA IOL) with CyA-CS-NP.Methods The CS-NP and CyA-CS-NP were prepared by ionic gelation of CS with sodium tripolyphosphate.The characteristics of CS-NP,such as the appearance and mean size,and drug entrapment efficient (EE),loading capacity (LC),and the drug release were studied ; the CyA content on the IOL surface was detected by high performance liquid chromatography (HPLC).The IOL surface modified with CyA-CS-NP was observed by scanning electron microscope and X-ray photoelectron spectroscopy technique (XPS),the changes of elements and chemical bond types between simple plasma processed IOL and CyA-CS-NP modified IOL were analyzed.The transmittance at the wavelength of 360-490 nm and refraction of IOL were detected using back focal length method and spectrophotometer,and the effective resolution of IOL was evaluated according to the instruction of ISO/CD 11979-2.Loops anti fatigue test of IOL referred to the criteria of ISO/CD 11979-3.Results The CS-NP and CyA-CS-NP showed monodisperse,uniform appearance similar to spherical shape with a mean size of (158±18) nm and (219±29) nm,respectively.The CyA-CS-NP had high CyA association efficiency and loading capacity (64.2％ and 7.6％).In vitro release study revealed a fast release on the first day followed by a increased drug release during an 11-day following up.The sustained release was approximately 46.6％ at day 1 and 77.7％ at day 12,respectively.The surface of IOLs with cling film was smooth without CS-NP;while the edge of IOLs appeared a layer of CyA-CS-NP after modification.XPS analysis displayed some elements such as phosphonium,CNH2 and O =CN that appeared on the modified surface,indicating that CyA-CS-NP existed on the surface of IOLs edge.The mean quality of CyA on three IOLs surface after modification was 171.88 μg.The diopter,distinguishing ability and transmittance of modified IOL were (16.64±0.23) D,(90.28 ± 0.25) ％ and (73.57 ±0.62) ％,and those of unmodified IOL were (16.62±0.29) D,(90.28±0.21) ％,(73.61±0.60)％,without significant differences between them (t =0.381,0.078,2.291,all at P ＞ 0.05).The antifatigue ability of loops complied with the criteria of ISO/CD 11979-3.Conclusions The optical property and antifatigue ability of loops of the edge-modified IOLs by CyA-CS-NP reach the normal standard and meet the requirement of clinic application.The edge-modified IOLs by CyA-CS-NP can be a delivery system for intraocular drug release.

Formulation design of Aceclofenac microcapsules by inotropic gelation technique, characterization studies and release kinetics.

Osteoarthritis predominantly affects the large weight bearing joints and the clinical characteristics include morning stiffness of short duration, stiffness or gelling on rest, pain on use, joint inflammation and bone deformity. Microcapsules of aceclofenac were formulated with methyl cellulose, sodium CMC and hydroxyl propyl methyl cellulose by technique. The microcapsules showed excellent rheological properties for all batches. The formulations showed drug content uniformity with high drug entrapment efficiency. The in vitro wash off test revealed the mucoadhesive ability of the micro capsules. Scanning electron microscopy indicated structural and surface morphology uniformity. The in vitro release studies indicated sustained release of aceclofenac from the formulations. Kinetic study of the release data indicated the zero order release and non fickian sustained release mode of drug release. The microcapsules showed the correlation between wall thickness and drug release pattern.