Progesterone release from glutaraldehyde cross-linked casein microspheres: In vitro studies and in vivo response in rabbits

Latha, M.S.; Lal, Arthur Vijayan; Kumary, T. V.; Sreekumar, RC; Jayakrishnan, A.

doi:10.1016/s0010-7824(00)00113-x

Cited by 74 publications

(49 citation statements)

References 17 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In a previous work, ascorbyl palmitate was more easily released from TPP-crosslinked chitosan nanoparticles at low TPP concentration because of the low-density structure. 36 Previous studies showed a sustained-release ability of drugs (eg, mitoxantrone 37 and progesterone 38 ) from glutaraldehyde-crosslinked CAS microparticles, where the rate of drug release was found to decrease with the increase in the glutaraldehyde concentration.…”

Section: In Vitro Release Of Flt From Cas Nanoparticlesmentioning

confidence: 99%

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Elzoghby¹,

Helmy²,

Samy³

et al. 2013

IJN

View full text Add to dashboard Cite

A novel particulate delivery matrix based on ionically crosslinked casein (CAS) nanoparticles was developed for controlled release of the poorly soluble anticancer drug flutamide (FLT). Nanoparticles were fabricated via oil-in-water emulsification then stabilized by ionic crosslinking of the positively charged CAS molecules below their isoelectric point, with the polyanionic crosslinker sodium tripolyphosphate. With the optimal preparation conditions, the drug loading and incorporation efficiency achieved were 8.73% and 64.55%, respectively. The nanoparticles exhibited a spherical shape with a size below 100 nm and a positive zeta potential (+7.54 to +17.3 mV). FLT was molecularly dispersed inside the nanoparticle protein matrix, as revealed by thermal analysis. The biodegradability of CAS nanoparticles in trypsin solution could be easily modulated by varying the sodium tripolyphosphate crosslinking density. A sustained release of FLT from CAS nanoparticles for up to 4 days was observed, depending on the crosslinking density. After intravenous administration of FLT-CAS nanoparticles into rats, CAS nanoparticles exhibited a longer circulation time and a markedly delayed blood clearance of FLT, with the half-life of FLT extended from 0.88 hours to 14.64 hours, compared with drug cosolvent. The results offer a promising method for tailoring biodegradable, drug-loaded CAS nanoparticles as controlled, long-circulating drug delivery systems of hydrophobic anticancer drugs in aqueous vehicles.

show abstract

Section: In Vitro Release Of Flt From Cas Nanoparticlesmentioning

confidence: 99%

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Elzoghby¹,

Helmy²,

Samy³

et al. 2013

IJN

View full text Add to dashboard Cite

show abstract

“…Biopolymer micro and nanoparticles have been proposed as an alternative to encapsulate progesterone (JAMEELA et al, 1998;LEMOS-SENNA et al, 1998;MATSUMOTO et al, 1999;LATHA et al, 2000;SILVA et al, 2006;SALEM, 2010). It is worth noting that besides the controlled delivery, encapsulation also provides protection from premature degradation during handling and storage before use, enhancement of absorption and bioavailability, improved retention time inside the organism and improvement of intracellular penetration (KUMARI et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Characterization of progesterone loaded biodegradable blend polymeric nanoparticles

et al. 2015

View full text Add to dashboard Cite

The encapsulation of progesterone in poly (hydroxybutirate-co-hydroxyvalerate) (PHBV), poly (ε-caprolactone) (PCL), poly (L-lactic acid) (PLLA) nanoparticles and PHBV/PCL and PHBV RESUMO A encapsulação de progesterona em nanopartículas de poli (hidroxibutirato-co-hidroxivalerato) (PHBV), poli (ε-caprolactona) (PCL), poli (L-ácido lático) (PLLA) e em nanopartículas blenda de PHBV/PCL e PHBV

show abstract

“…24 In the case of casein, microspheres cross-linked with glutaraldehyde have been used for progesterone release . 20 In this study, our particular interest was to analyze the permeation rate of p-hydroxyacetanilide (a model drug) through gelatin/caseins films cross-linked with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC). The permeation behavior was evaluated considering the thermal, mechanical, morphologic, and water absorption properties of the cross-linked system.…”

Section: Introductionmentioning

confidence: 99%

“…18 In general, p-hydroxyacetanilide is effective with ingested doses ranging between 0.5 -1.0 g every 3 or 4 h. Considering that this causes inconvenience to the patient, many polymeric systems have been tested as new ways to control the release of different drugs. [19][20][21][22][23][24] Investigations have been carried out in order to obtain an ideal model for drug delivery with high specificity and activity without toxic effects. 25 Along with several drug delivery systems using membrane-controlled diffusion, films and membranes for transdermal delivery have also been studied.…”

mentioning

confidence: 99%

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

Cristiano¹,

Fayad²,

Porto³

et al. 2010

J. Braz. Chem. Soc.

View full text Add to dashboard Cite

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...

show abstract

Progesterone release from glutaraldehyde cross-linked casein microspheres: In vitro studies and in vivo response in rabbits

Cited by 74 publications

References 17 publications

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Characterization of progesterone loaded biodegradable blend polymeric nanoparticles

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

Contact Info

Product

Resources

About