Surface and transport properties of acrylic polymers influencing drug release from porous matrices

Carli, F.; Capone, G.; Colombo, I.; Magarotto, Lorenzo; Motta, Alessandro

doi:10.1016/0378-5173(84)90190-x

Cited by 35 publications

(13 citation statements)

References 19 publications

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“…In contrast, drug release from polymethacrylate-based tablets was complete due to their inherent water permeability, allowing drug diffusion to occur through the hydrated polymeric network. This was confirmed by Carli et al who reported that drug release form Eudragit RL-or RS-based systems was controlled by intraparticle diffusion (27). Drug release from matrix tablets based on Eudragit RL and RS was not affected by TEC content (0-10%).…”

Section: In Vitro Drug Releasesupporting

confidence: 73%

Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding

et al. 2012

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Abstract. Sustained-release matrix tablets based on Eudragit RL and RS were manufactured by injection moulding. The influence of process temperature; matrix composition; drug load, plasticizer level; and salt form of metoprolol: tartrate (MPT), fumarate (MPF) and succinate (MPS) on ease of processing and drug release were evaluated. Formulations composed of 70/30% Eudragit RL/MPT showed the fastest drug release, substituting part of Eudragit RL by RS resulted in slower drug release, all following first-order release kinetics. Drug load only affected drug release of matrices composed of Eudragit RS: a higher MPT concentration yielded faster release rates. Adding triethyl citrate enhanced the processability, but was detrimental to long-term stability. The process temperature and plasticizer level had no effect on drug release, whereas metoprolol salt form significantly influenced release properties. The moulded tablets had a low porosity and a smooth surface morphology. A plasticizing effect of MPT, MPS and MPF on Eudragit RS and Eudragit RL was observed via DSC and DMA. Solubility parameter assessment, thermal analysis and X-ray diffraction demonstrated the formation of a solid solution immediately after production, in which H-bonds were formed between metoprolol and Eudragit as evidenced by near-infrared spectroscopy. However, high drug loadings of MPS and MPF showed a tendency to recrystallise during storage. The in vivo performance of injection-moulded tablets was strongly dependent upon drug loading.

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Section: In Vitro Drug Releasesupporting

confidence: 73%

Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding

et al. 2012

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“…The n values from Korsmeyer equation lower than 0.45 (Ritger & Peppas, 1987) and the prevalence of k d and the negative values for k r in Peppas equation reveals a drug release mechanism controlled mainly by drug diffusion (Colombo, Bettini, Catellani, Santi, & Peppas, 1999). Different authors (Carli, Capone, & Colombo, 1984;Colombo, Conte, Caramella, Gazzaniga, & La Manna, 1985;Farhadieh, Borodkin, & Buddenhagen, 1971) have also postulated a diffusion mechanism when evaluating the drug release mechanism from matrices obtained from acrylic/methacrylic copolymers.…”

Section: Mixturesmentioning

confidence: 95%

Graft tapioca starch copolymers as novel excipients for controlled-release matrix tablets

Casas

Ferrero

Jiménez-Castellanos

2010

Carbohydrate Polymers

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“…The surface activity of amphiphilic polymers determines their interaction with the solid surface at the interface with liquid or air and dictates their applications in pharmaceutical formulations and drug delivery 17, 18. Contact angle measurement is a simple, useful and very sensitive method for investigation of interfacial phenomena and estimation of interfacial energy 19–23.…”

Section: Introductionmentioning

confidence: 99%

Characterization of novel soybean‐oil‐based thermosensitive amphiphilic polymers for drug delivery applications

Abdekhodaie

Liu

Erhan

et al. 2012

Polymer International

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Hydrolyzed polymers of soybean oil (HPSO) and of epoxidized soybean oil (HPESO) were developed previously. Owing to their natural food origin and biocompatibility, we exploited further their potential as a drug delivery system and pharmaceutical excipients. This work aimed to investigate self-assembly, thermal transition, interaction with various drugs and surface activity of these novel amphiphilic polymers. The critical micelle concentration of HPSO and HPESO was determined by the surface tension method. The molecular interaction between HPESO and anticancer drug doxorubicin HCl was examined. The effect of the polymers on the solution contact angle and surface energy of compressed tablets of hydrophobic drugs ibuprofen and nifedipine was measured. The thermal transition temperatures T tr (cloud points) of the polymers in aqueous solutions increased with increasing polymer concentration. HPSO exhibited lower T tr than HPESO. The critical micelle concentration was found to be 0.05 mg mL −1 for HPSO and 0.08 mg mL −1 for HPESO. Strong molecular interactions between HPESO and doxorubicin were observed. Both polymers reduced the interfacial energy and contact angles of drug tablets with more effect on ibuprofen tablets with the use of HPSO. These results suggest that the novel soybean-oil-based amphiphilic polymers have great potential for drug delivery and pharmaceutical formulations.

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Surface and transport properties of acrylic polymers influencing drug release from porous matrices

Cited by 35 publications

References 19 publications

Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding

Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding

Graft tapioca starch copolymers as novel excipients for controlled-release matrix tablets

Characterization of novel soybean‐oil‐based thermosensitive amphiphilic polymers for drug delivery applications

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