Factors influencing the diffusion-controlled release of papaverine from poly (l-lactic acid) matrix

Miyajima, Makoto; Koshika, Akiko; Okada, Junichi; Kusai, Akira; Ikeda, Miyoshi

doi:10.1016/s0168-3659(98)00076-5

Cited by 80 publications

(41 citation statements)

References 19 publications

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“…These phenomena depend upon the interaction between the dissolution media, polymeric matrix and drug (3) and are influenced by several formulation variables, which include but are not limited to the drug concentration, drug solubility, polymer particle size (5,(8)(9)(10), drug to polymer mass ratio, polymer viscosity, polymer molecular mass (3,4,10) and the addition of different types and levels of formulation excipients (1,(11)(12)(13)(14)(15).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the Impacts of Formulation Variables and Excipients on the Drug Release Dynamics of a Polyamide 6,10-Based Monolithic Matrix Using Mathematical Tools

et al. 2013

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Abstract. Drug release from hydrophilic matrices is regulated mainly by polymeric erosion, disentanglement, dissolution, swelling front movement, drug dissolution and diffusion through the polymeric matrix. These processes depend upon the interaction between the dissolution media, polymeric matrix and drug molecules, which can be significantly influenced by formulation variables and excipients. This study utilized mathematical parameters to evaluate the impacts of selected formulation variables and various excipients on the release performance of hydrophilic polyamide 6,10 (PA 6,10) monolithic matrix. Amitriptyline HCl and theophylline were employed as the high and low solubility model drugs, respectively. The incorporation of different excipient concentrations and changes in formulation components influenced the drug release dynamics as evidenced by computed mathematical quantities (t x% , MDT x%, f 1 , f 2 , k 1 , k 2 , and К F ). The effects of excipients on drug release from the PA 6,10 monolithic matrix was further elucidated using static lattice atomistic simulations wherein the component energy refinements corroborates the in vitro and in silico experimental data. Consequently, the feasibility of modulating release kinetics of drug molecules from the novel PA 6,10 monolithic matrix was well suggested.

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Section: Introductionmentioning

confidence: 99%

Evaluation of the Impacts of Formulation Variables and Excipients on the Drug Release Dynamics of a Polyamide 6,10-Based Monolithic Matrix Using Mathematical Tools

et al. 2013

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“…This is in agreement with other studies reporting that high crystallinity of the matrix may have a negative influence on the release rate of a drug, because the lamellae may act as a barrier during drug diffusion. 18,37,38 Bigger and more perfectly shaped crystalline lamellae should reduce overall release of the drug. This is probably the reason for higher release rates in the case of PPAz and PPPim, which show a low degree of crystallinity, ie, 29.5% and 42.6% respectively.…”

mentioning

confidence: 99%

Evaluating the effects of crystallinity in new biocompatible polyester nanocarriers on drug release behavior

Karavelidis¹,

Karavas²,

Giliopoulos³

et al. 2011

IJN

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Four new polyesters based on 1,3-propanediol and different aliphatic dicarboxylic acids were used to prepare ropinirole HCl-loaded nanoparticles. The novelty of this study lies in the use of polyesters with similar melting points but different degrees of crystallinity, varying from 29.8% to 67.5%, as drug nanocarriers. Based on their toxicity to human umbilical vein endothelial cells, these aliphatic polyesters were found to have cytotoxicity similar to that of polylactic acid and so may be considered as prominent drug nanocarriers. Drug encapsulation in polyesters was performed via an emulsification/solvent evaporation method. The mean particle size of drug-loaded nanoparticles was 164–228 nm, and the drug loading content was 16%–23%. Wide angle X-ray diffraction patterns showed that ropinirole HCl existed in an amorphous state within the nanoparticle polymer matrices. Drug release diagrams revealed a burst effect for ropinirole HCl in the first 6 hours, probably due to release of drug located on the nanoparticle surface, followed by slower release. The degree of crystallinity of the host polymer matrix seemed to be an important parameter, because higher drug release rates were observed in polyesters with a low degree of crystallinity.

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“…The ability to diffuse into the surrounding medium as well as the release kinetics of a drug that has been loaded in a polymeric carrier depend on various factors, including the solubility and the possibility of swelling of the polymeric matrix in the medium according to Tungprapa et al [15]. Moreover, when a pharmaceutical agent is loaded inside a biodegradable polymeric carrier, two distinct major mechanisms are known to facilitate the drug release, mainly polymer degradation and small molecule diffusion [16]. PCL displays little degradation in aqueous environment during the first months [8], whereas PEG is a water soluble polymer that can be immediately dissolved in the surrounding medium.…”

Section: Introductionmentioning

confidence: 99%

Pcl/Peg Electrospun Fibers as Drug Carriers for the Controlled Delivery of Dipyridamole

Repanas¹,

Wf²,

O³

et al. 2015

J In Silico In Vitro Pharmacol

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Electrospinning is a versatile and diverse technology for the production of nano-and microfibers that can be used as a drug delivery system (DDS). The aim of this study was to create fibrous scaffolds from a mixture of polycaprolactone (PCL) and polyethylene glycol (PEG) and to evaluate the suitability of the fibers as DDS. Dipyridamole (DPA), an anti-thrombotic and anti-proliferative pharmaceutical agent, was used as a model drug. Two types of PEG with different chain length were used. The structural, mechanical and physicochemical characteristics of the fibers with and without DPA, were determined, and the release kinetics of DPA were studied. The obtained fibers loaded with DPA and with the higher molecular weight PEG were smooth and had an average diameter of 586.75 ± 204.79 nm and an average Young's modulus of 57.14 ± 4.35 MPa, whereas the tensile strain at break was 0.61 ±0.05 mm/mm and the ultimate tensile strength (UTS) was 16.79 ± 3.08 MPa. The cumulative release of DPA revealed two stages: an initial burst phenomenon followed by slower Fickian diffusion (release exponent n = 0.432).

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Factors influencing the diffusion-controlled release of papaverine from poly (l-lactic acid) matrix

Cited by 80 publications

References 19 publications

Evaluation of the Impacts of Formulation Variables and Excipients on the Drug Release Dynamics of a Polyamide 6,10-Based Monolithic Matrix Using Mathematical Tools

Evaluation of the Impacts of Formulation Variables and Excipients on the Drug Release Dynamics of a Polyamide 6,10-Based Monolithic Matrix Using Mathematical Tools

Evaluating the effects of crystallinity in new biocompatible polyester nanocarriers on drug release behavior

Pcl/Peg Electrospun Fibers as Drug Carriers for the Controlled Delivery of Dipyridamole

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