Controlled release of anticancer drug methotrexate from biodegradable gelatin microspheres

Narayani, Raj I.; Rao, K. Panduranga

doi:10.3109/02652049409040439

Cited by 80 publications

(25 citation statements)

References 7 publications

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“…This proteinaceous material has the amino acid sequence and functional groups of proteins, as well as the random coil conformation and molecular flexibility of a water-soluble polymer. Gelatin cross-linking has been investigated in solubility issues of gelatin capsules, 8 in formation of microspheres, 9 and for insight into the cross-linking process itself. 10 Gelatin reactions with EDC have been used in this laboratory for gelatin modification and cross-linking, 11 synthesis of anticancer drug conjugates, 12,13 and evaluation of drug conjugate properties on cytotoxicity.…”

Section: Introductionmentioning

confidence: 99%

Carbodiimide Induced Cross-Linking, Ligand Addition, and Degradation in Gelatin

2015

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The water-soluble carbodiimide, 1-ethyl-3-(3-(dimethylaminopropyl)-carbodiimide (EDC) is widely used in protein chemistry. We used EDC-induced gelatin cross-linking as a model for amide bond formation to resolve reaction ambiguities with common variables of buffers, gelatin concentration, and pH. Percentage changes in SEC high molecular weight peak areas were used to follow the reactions. Differences in reaction rate and extent were observed with four commonly used buffers, while differences in extent were observed for commonly used concentrations and pH. We also investigated an anhydride mechanism for aqueous EDC-induced amide bond formation that has received little attention since its proposal in 1995. Gelatin carboxyl groups had a synergistic role during the addition of hydrazine to corroborate the anhydride formation between carboxyl groups. EDC-induced degradation of gelatin was investigated using percentage changes in SEC low molecular weight peak areas. The degradation occurred in excess EDC at neutral to alkaline pH and was enhanced substantially when reacting amino groups were not available. A mechanism of EDC-induced gelatin degradation is proposed and designated the extended Khorana mechanism. This EDC side reaction has the potential to occur in peptides and proteins under similar conditions.

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Section: Introductionmentioning

confidence: 99%

Carbodiimide Induced Cross-Linking, Ligand Addition, and Degradation in Gelatin

2015

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“…20 s), add 20 ml of acetone with continuous stirring for 5 h. The microspheres formed were washed with acetone five times and with water three times and then dried in a vacuum desiccator to get free-flowing microspheres in a powder form. By varying the drug:polymer ratio, six batches of microspheres were prepared [9][10][11] [ Table 1]. …”

Section: Preparation Of Microspheres Of Mtxmentioning

confidence: 99%

Preparation and evaluation of biodegradable microspheres of methotrexate

Halith¹,

Firthouse²,

Kulaturanpillai³

et al. 2009

Asian J Pharm

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T he objective of the present study is to prepare sustained-release methotrexate microspheres of bovine serum albumin in different ratios by the emulsion cross-linking method. The prepared microspheres were subjected to various physicochemical evaluation and in vitro release studies. The drug release from microspheres of 1:6 ratio is the most constant and prolonged drug release is diffusion followed by erosion. The characteristics of the prepared microspheres are conducive to the formulation of the sustained release drug delivery system.

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“…Another study reports the preparation of gelatin microspheres by polymer dispersion technique and cross-linked with GA. They had an 80 % loading of MTX and showed a zero-order fashion for ~ 6 days in SGF, and from 5 to 8 days in SIF being slower in SIF (Narayani 1994(Narayani , 1995. Another study reports the possible involvement of the primary amino group of doxorubicin (DXR) in the cross-linking process of gelatin nanoparticles.…”

Section: Cross-linking Of Gelatinmentioning

confidence: 99%

Improved Polymer Functionality by Cross-linking with Glutaraldehyde to Achieve Controlled Drug Release

Rojas

2015

Excipient Applications in Formulation Design and Drug Delivery

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There are many approaches to combine drug and polymers. One of them involves the use of drug-polymer conjugates in which the drug is covalently bounded to a polymer through a hydrolyzable linkage. However, the most widely used approach involves polymers as matrixes in which the drug and polymer are mixed physically and the release is achieved by diffusion from the surrounding polymeric matrix or by disintegration of the polymeric matrix. Nevertheless, most biopolymers per se do not possess adequate physicochemical and mechanical properties to produce a film or hydrogel which can be used as a matrix for the controlled release of drugs. For this reason, many cross-linking agents have been used to improve these polymer properties. The most reactive and typical cross-linking agent employed is glutaraldehyde. This chapter discusses the modification of drug release properties of polymers suchs as poly(vinyl) alcohol, chitosan, gelatin, alginates, carrageenan and naturally occurring gums by chemical modification via glutaraldehyde cross-linking. Most cross-linked products are more amorphous due to the reduction of the hydroxyl network responsible for cross-linking, crystallinity and water interaction.

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Controlled release of anticancer drug methotrexate from biodegradable gelatin microspheres

Cited by 80 publications

References 7 publications

Carbodiimide Induced Cross-Linking, Ligand Addition, and Degradation in Gelatin

Carbodiimide Induced Cross-Linking, Ligand Addition, and Degradation in Gelatin

Preparation and evaluation of biodegradable microspheres of methotrexate

Improved Polymer Functionality by Cross-linking with Glutaraldehyde to Achieve Controlled Drug Release

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