Preparation and characterization of β‐cyclodextrin‐linked chitosan microparticles

Hydrophobically modified chitosan containing β‐cyclodextrin (CD) units was synthesized by using tosylated β‐CD. The final product was characterized by Fourier transform infrared (FTIR) spectroscopy, elemental analysis and TGA, and rheometry. The polymer bearing β‐CD moieties was used to obtain crosslinked microparticles by spray‐drying which could then be used in a controlled release system for drugs. FTIR confirmed the formation of an amide linkage between cyclodextrin and chitosan. As fluorescence spectroscopy demonstrated, hydrophobic microenvironments were formed by chitosan bearing cyclodextrin in solution at lower concentrations than for chitosan. Rheometry and FTIR showed the crosslinking of the new polymer using genipin, a molecule of natural origin. Microspheres (MS) obtained by spray‐drying showed narrow size distribution when β‐CD was grafted onto chitosan and ξ‐potential of MS was slightly lower although it remained positive. In conclusion, β‐CD linked chitosan polymer can be considered as a very promising controlled drug delivery system for drugs. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

Formulation studies for mirtazapine orally disintegrating tablets

Abstract

Objective: Orally disintegrating tablets (ODTs) recently have gained much attention to fulfill the needs for pediatric, geriatric, and psychiatric patients with dysphagia. Aim of this study was to develop new ODT formulations containing mirtazapine, an antidepressant drug molecule having bitter taste, by using simple and inexpensive preparation methods such as coacervation, direct compression and to compare their characteristics with those of reference product (Remereon SolTab).

Materials and methods: Coacervation method was chosen for taste masking of mirtazapine. In vitro characterization studies such as diameter and thickness, weight variation, tablet hardness, tablet friability and disintegration time were performed on tablet formulations. Wetting time and in vitro dissolution tests of developed ODTs also studied using 900?mL 0.1?N HCl medium, 900?mL pH 6.8 phosphate buffer or 900?mL pH 4.5 acetate buffer at 37?±?0.2?°C as dissolution medium.

Results: Ratio of Eudragit® E-100 was chosen as 6% (w/w) since the dissolution profile of A1 (6% Eudragit® E-100) was found closer to the reference product than A2 (4% Eudragit® E-100) and A3 (8% Eudragit® E-100). Group D, E and F formulations were presented better results in terms of disintegration time. Dissolution results indicated that Group E and F formulations showed optimum properties in all three dissolution media.

Discussion: Formulations D1, D4, D5, E3, E4, F1 and F5 found suitable as ODT formulations due to their favorable disintegration times and dissolution profiles.

Conclusion: Developed mirtazapine ODTs were found promising in terms of showing the similar characteristics to the original formulation.     

Preparation and optimisation of liposome‐in‐alginate beads containing oyster hydrolysate for sustained release

Oyster (Crassostrea gigas) hydrolysate shows antihypertensive effect in our previous study. Oral administration of oyster hydrolysate can loss bioactive peptides due to enzymatic degradation in vivo. To maximise its bioavailability, liposome‐in‐alginate (LA) beads were used to encapsulate the oyster hydrolysates to protect from degradation and obtain sustained release. The preparation conditions of the LA beads were optimised by response surface method using a model peptide of tyrosylalanine (YA). Their characterisation, swelling and release properties were investigated. The optimised conditions for the concentration of calcium chloride, sodium alginate and the amount of ethanol‐dissolved lecithin (EDL) were 0.5 m , 3% and 95.4 mg, respectively. The encapsulation efficiencies of YA and the oyster hydrolysate in the optimised condition were 74.9% and 84.3%, respectively. The release time of the oyster hydrolysate in the simulated gastrointestinal fluid was up to 16 h. The LA beads can be recommended to encapsulate oyster hydrolysate for bioavailability improvement.     

Effect of microencapsulation and spray drying on oxidative stability of flaxseed oil and its release behavior under simulated gastrointestinal conditions

Flaxseed oil is one of the richest sources of omega-3 fatty acid (α-linolenic acid, ALA). It contains high amounts of polyunsaturated fatty acids, making it extremely susceptible to oxidation. In the present study, flaxseed oil was stabilized using microencapsulation followed by spray drying and studied for its oxidative stability in terms of peroxide value (PV), thiobarbituric acid, and p-anisidine value at room temperature (35 ± 1°C) and low temperature (4–7°C) storage for 6 months. Results revealed that the developed flaxseed oil powder was stable throughout the storage period and PV remained below to the maximum permissible limit (≤5 mEq/kg oil) prescribed by the Codex Alimentarius Commission. The fatty acids profile measured by gas–liquid chromatography indicated a 14.28–15.13% decrease in ALA content in flaxseed oil as a result of microencapsulation and storage at room temperature. In vitro digestion behavior of microcapsules showed 4.39 ± 0.53 to 19.87 ± 0.47% release of flaxseed oil under simulated gastric continued, whereas under gastrointestinal conditions it was 20.00 ± 3.66 to 59.99 ± 9.29%.     

Robust microencapsulated phase change materials in concrete mixes for sustainable buildings

For passive building applications, phase change materials (PCMs) are microencapsulated to avoid leakage of PCM from concrete structure. The primary challenge of using microencapsulated PCM (MPCM) is its weak shell structure. New MPCMs with different shell compositions to prevent breakage during mixing in fresh concrete are needed. In this study, free radical polymerization method to microencapsulate capric acid–myristic acid mixture as PCM with two different methyl methacrylate co‐polymers is proposed to produce robust MPCMs for building applications. Two new microcapsules (MPCM‐1 and MPCM‐2) having latent heats of 91.9 and 97.3 J/g were synthesized. SEM analyses showed the size of microcapsules being in the range of 400–850 nm for MPCM‐1 and 250–475 nm for MPCM‐2. Analyses also reveal that the shells of MPCMs were not harmed, as they were added into concrete mixes. The microsphere's geometry was preserved, and distribution was homogeneous. The MPCMs were also studied under thermal tests of 1000 heating/cooling cycles. No significant changes in thermal properties were observed after thermal cycling tests. Copyright © 2016 John Wiley & Sons, Ltd.     

杀螟硫磷微胶囊化的研究

本研究将水相复凝聚相分离工艺应用于杀螟硫磷的微胶囊化，并对工艺条件进行了探讨。结果表明ＰＨ值，固化剂用量，乳化剂用量和防粘剂用量对微胶囊的制备有很大影响。     

Preparation and characterization of crosslinked chitosan microspheres for the colonic delivery of 5-fluorouracil

In this work, we attempted to develop a simple and inexpensive colon specific pulsatile drug-delivery system using chitosan microspheres loaded with 5-fluorouracil (5-FU) using an enteric-coated soft gelatin capsule. Chemical crosslinking by glutaraldehyde and interactions between the polymer and the drug were determined by Fourier transform infrared spectral study. Scanning electron microscopy of the microspheres revealed spherical shapes with smooth surfaces. Differential scanning calorimetry studies confirmed the molecular dispersion of the drug in the polymer matrix. Three different formulations (i.e., F1, F2, and F3) were prepared by the variation of the amount of 5-FU. Encapsulation efficiencies of 5.5, 10.8, and 17.9% for drug loadings of 10, 20, and 50%, respectively, were obtained. In vitro release studies were conducted at pH 1.2 and pH 7.4 (to simulate actual gastrointestinal fluid and gastrointestinal tract conditions, respectively). The results indicate that chitosan microspheres released 5-FU in both acidic (60%) and basic pH (40%) conditions, whereas the capsule (filled with chitosan microspheres) showed only 8–10% release in acidic media and nearly 90% in basic media within 12 h. The newly designed pulsatile capsule device could be used for targeting 5-FU to the colon. © 2012 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

Core content and stability of n‐octadecane‐containing polyurea microencapsules produced by interfacial polymerization

Microencapsulation of phase change material (PCM) n‐octadecane was carried out by interfacial polymerization technique using core and bulk monomers as toluene‐2,4‐diisocyanate (TDI) and diethylene triamine (DETA), respectively. Cyclohexane was used as the solvent for TDI and n‐octadecane, which formed the oil phase. The effect of encapsulation procedure, core‐to‐monomer ratio (CM ratio) and PCM‐to‐cyclohexane (PC) ratio was investigated on core content, encapsulation efficiency, and stability of microcapsules. Using a modified procedure, the core content was found to increase with the increasing CM ratio and reached a maximum at 3.7, while the encapsulation efficiency continuously decreased with the increasing CM ratio. Also the encapsulation efficiency was found to have a strong dependence on PC ratio and a maximum encapsulation efficiency of 92%, along with the core content of 70% was obtained with CM ratio of 3.7 along with the PC ratio of 6. The microcapsules were well shaped, i.e., round and regular, with narrow size distribution at these conditions. The PCM microcapsules were found to be stable to heat treatment at 150°C for 8 h. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2007     

Microwave-assisted encapsulation of citric acid using hydrocolloids

This study elucidates the capability of a novel technique for producing microcapsules at an enormously short time and low cost. This technique is based on the difference between dielectric constants of core and coat materials. Edible citric acid was mixed with various biomacromolecules at ratios of 1:5, 1:10, and 1:100. Each mixture was treated up to 600 s at various powers (120–1200 W) in a microwave oven. Subsequently, the microcapsules were separated by distinct sieves, and their apparent structure and quality were evaluated using binoculars, and photographs were taken for visual comparisons. Our observations showed that only five hydrocolloids were able to produce high-quality and efficient encapsulation [casein > inulin > carboxymethylcellulose (CMC) > low methoxyl (LM) pectin (9/5%) > sorbitol]. Moreover, the highest coating efficiency was seen at highest intensity (1200 W) at a mixing ratio of 1:10. Furthermore, the optimum treating time periods for those five efficient coating materials were about 400, 75, 400, 100, and 100 s.     

阻燃剂新品种——微胶囊化TBC及其应用

采用微胶囊包覆的方法提高了三－（２，３－二溴丙基）异氰尿酸酯（ＴＢＣ）的热稳定性，对这种阻断剂新品种的制备方法，性质和用途做了介绍。