Protein-based films cross-linked with 1-ethyl-3-(3-dimethylamino-propyl) carbodiimide hydrochloride (EDC): effects of the cross-linker and film composition on the permeation rate of p-hydroxyacetanilide as a model drug

Abstract

Filmes reticulados de gelatina (Gel), caseína (Cas) e a mistura Gel/Cas (1:1, m/m) foram estudados em termos das propriedades térmicas, morfológicas e absorção de água e quanto ao perfil de permeação de p-hidroxiacetanilida (p-HAA ) como fármaco modelo. O grau de reticulação por 1-etil-3-(3-cloridrato) dimetilaminopropil carbodiimida (EDC) foi de 90,6% para filmes de Gel e cerca de 70% para filmes de Cas e misturas Gel/Cas (1:1, m/m). A total solubilidade dos filmes não-reticulados foi reduzida para somente 21 -22% após reticulação com EDC. Apesar do alto grau de reticulação, o intumescimento dos filmes de Gel (87,2%) foi praticamente o dobro do determinado para filmes de Gel/Cas (1:1, m/m) e Cas. A taxa de permeação de p-HAA seguiu a ordem Gel > Gel/Cas @ Cas para filmes reticulados, ou seja, um comportamento consistente com o maior intumescimento da Gel em relação aos outros dois sistemas estudados. Os menores valores de permeação observados para filmes de Cas e Gel/Cas, sugerem que estes sistemas podem ser utilizados para controlar a permeação de fármacos. Considerando os diferentes modelos matemáticos aplicados, os sistemas estudados não mostraram um bom ajuste relativamente a equação de primeira ordem e somente uma parcial correlação com as equações de ordem zero e do modelo de Higuchi. No entanto, uma boa correlação (r 2 > 0,99) foi obtida utilizando a equação da lei das potências (valores de n = 0,70 -0,87), indicando que a permeação de p-HAA através dos filmes foi controlada principalmente pelo mecanismo de difusão.Cross-linked films of gelatin (Gel), casein (Cas) and their (1:1, m/m) mixture (Gel/Cas) were studied in terms of their thermal, morphological and water absorption properties and the permeation profile of p-hydroxyacetanilide (p-HAA) as a model drug. The degrees of cross-linking by 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) were 90.6% for Gel films and approximately 70% for Cas and Gel/Cas films. The totally soluble non cross-linked films achieved only 21 -22% of solubility after cross-linking with EDC. Despite the high cross-linking degree, the swelling of Gel films (87.2%) was practically twice that determined for Gel/Cas and Cas films. The permeation rate of p-HAA followed the order Gel > Gel/Cas @ Cas for cross-linked films, which is consistent with the Gel film showing a greater swelling than the other two systems studied. Lower permeation rates were observed for Cas and Gel/Cas films, suggesting that these could be used as rate-controlling systems for drug permeation. For the different mathematical models applied, the systems studied did not show a good fit with the first-order equation and only a partial fit with the zero-order equation and Higuchi's model. However, good correlations (r 2 > 0.99) were obtained using the power law equation (n = 0.70 -0.87), indicating that the p-HAA permeation through the films was mainly controlled by a diffusion mechanism.Keywords: gelatin, casein, films, cross-linking, drug permeation Introduction Gelatin (Gel), which is obtain...

Preparation, characterization and properties of films obtained from cross-linked guar gum

“…The cross-linking process in films generally increases the TS and decreases the percentage of elongation. However, the opposite behavior observed in our case for the GG/EDC system is in agreement with results reported for other polysaccharide and protein systems [23,45] . The EDC interacts with hydroxyl groups from the backbone or from the galactose side group, blocking the hydrogen bonding sites on the guar gum and consequently reducing the intermolecular interactions between the polymer molecules.…”

Physico-Chemical Properties of Extruded Copolymer Film

“…Application of gelatine for food packaging can be improved by processing and physical or chemical modifications (Cristiano et al . ).…”

“…Apart from film formation, gelatine with maize starch and/or egg white can be used for producing composite gels (Tan et al 2015). Application of gelatine for food packaging can be improved by processing and physical or chemical modifications (Cristiano et al 2010).…”

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“…Gelatin, a protein derived from collagen and bones is translucent, colorless, brittle and tasteless, promotes general joint health and stiffness in athletes. It has good film forming property and known for its wound healing properties by preventing fluid loss due to exudation 13,[22][23][24][25][26] .…”