Polymeric hydrogels are widely used as controlled-release matrix tablets. In the present study, we investigated high-methoxy pectins for their potential value in controlled-release matrix formulations. The effects of compression force, ratio of drug to pectin, and type of pectin on drug release from matrix tablets were also investigated. The results of the in vitro release studies show that the drug release from compressed matrix tablets prepared from pectin can be modified by changing the amount and the type of pectin in the matrix tablets. However, compression force did not significantly affect the drug release. The mechanisms controlling release rate were discussed with respect to drug diffusion through the polymer matrices, but may be more complex.
Catechins are major antioxidants in green tea (Camellia sinensis or Camellia assamica), but because they do not permeate the skin well, the application of green tea in cosmetic products has so far been limited. This study aims to evaluate the cutaneous absorption of catechins from an extract of green tea and from a green tea extract-loaded chitosan microparticle. The catechin skin metabolism was also examined. The results suggest that chitosan microparticles significantly improve the ability of catechins to permeate skin. The cutaneous metabolism of the catechins significantly affected their permeation profiles. Epicatechin (EC) and epigallocatechin (EGC) penetrated the skin more than epigallocatechin gallate (EGCG) and epicatechin gallate (ECG). The galloyl groups in EGCG and ECG were enzymatically hydrolysed to EGC and EC, respectively. Dehydroxylation of catechins was also observed. Chitosan microparticles effectively prevented enzymatic changes of the catechins; therefore, chitosan microparticles are here found to be the promising carriers for enhancing the skin permeation.
INTRODUCTIONThe aim of this work was to assess the effect of 2 formulation variables, the pectin type (with different degrees of esterification [DEs]) and the amount of calcium, on drug release from pectin-based matrix tablets. Pectin matrix tablets were prepared by blending indomethacin (a model drug), pectin powder, and various amounts of calcium acetate and then tableting by automatic hydraulic press machine. Differential scanning calorimetry, powder x-ray diffraction, and Fourier transformed-infrared spectroscopy studies of the compressed tablets revealed no drug-polymer interaction and the existence of drug with low crystallinity. The in-vitro release studies in phosphate buffer (United States Pharmacopeia) and tris buffer indicated that the lower the DE, the greater the time for 50% of drug release (T 50 ). This finding is probably because of the increased binding capacity of pectin to calcium. However, when the calcium was excluded, the pectins with different DEs showed similar release pattern with insignificant difference of T 50 . When the amount of calcium acetate was increased from 0 to 12 mg/tablet, the drug release was significantly slower. However, a large amount of added calcium (ie, 24 mg/tablet) produced greater drug release because of the partial disintegration of tablets. The results were more pronounced in phosphate buffer, where the phosphate ions induced the precipitation of calcium phosphate. In conclusion, both pectin type and added calcium affect the drug release from the pectin-based matrix tablets.Hydrophilic polymer matrix systems are widely used in oral controlled drug delivery because of their flexibility to obtain a desirable drug release profile, cost-effectiveness, and broad regulatory acceptance. [1][2][3] The ability of the hydrophilic polymer matrices to release an entrapped drug in aqueous medium and to regulate the release of such drug by control of swelling and cross-linking makes them particularly suitable for controlled-release applications.2 These matrices can be applied for the release of both hydrophilic and hydrophobic drugs and charged solutes. Recently, many controlled-release formulations based on hydrophilic polymer matrices have been developed. [3][4][5][6] Pectins are hydrophilic polysaccharides derived from plant cell walls. They contain linear chains of (1→4) linked α-Dgalacturonic acid residues.7 These uronic acids have carboxyl groups, some of which are naturally presented as methyl esters. The degree of esterification (DE), which is expressed as a percentage of the esterified carboxyl groups, is an important means to classify pectins. High methoxy (HM) pectins (with DE >50%) require a relatively high concentration of soluble solids and a low pH for gel formation. [7][8] Low methoxy (LM) pectins (with DE <50%) form rigid gels by the action of calcium or multivalent cations, which cross-link the galacturonic acid chains. 7 The nontoxicity and the low production costs of pectins make them of great interest for the formulation of controlled-release do...
The aim of this work was to assess the effect of 2 formulation variables, the pectin type (with different degrees of esterification [DEs]) and the amount of calcium, on drug release from pectin-based matrix tablets. Pectin matrix tablets were prepared by blending indomethacin (a model drug), pectin powder, and various amounts of calcium acetate and then tableting by automatic hydraulic press machine. Differential scanning calorimetry, powder x-ray diffraction, and Fourier transformed-infrared spectroscopy studies of the compressed tablets revealed no drug-polymer interaction and the existence of drug with low crystallinity. The in-vitro release studies in phosphate buffer (United States Pharmacopeia) and tris buffer indicated that the lower the DE, the greater the time for 50% of drug release (T50). This finding is probably because of the increased binding capacity of pectin to calcium. However, when the calcium was excluded, the pectins with different DEs showed similar release pattern with insignificant difference of T50. When the amount of calcium acetate was increased from 0 to 12 mg/tablet, the drug release was significantly slower. However, a large amount of added calcium (ie, 24 mg/tablet) produced greater drug release because of the partial disintegration of tablets. The results were more pronounced in phosphate buffer, where the phosphate ions induced the precipitation of calcium phosphate. In conclusion, both pectin type and added calcium affect the drug release from the pectin-based matrix tablets.
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