A new mathematical model quantifying drug release from bioerodible microparticles using Monte Carlo simulations.

Abstract:

PURPOSE:The major objectives of this study were to 1) develop a new mathematical model describing all phases of drug release from bioerodible microparticles; 2) evaluate the validity of the theory with experimental data; and 3) use the model to elucidate the release mechanisms in poly(lactide-co-glycolide acid)-based microspheres. METHODS; 5-Fluorouracil-loaded microparticles were prepared with an oil-in-water solvent extraction technique and characterized in vitro. Monte Carlo simulations and sets of partial differential equations were used to describe the occurring chemical reactions and physical mass transport phenomena during drug release. RESULTS:The new mathematical model considers drug dissolution, diffusion with nonconstant diffusivities and moving boundary conditions, polymer degradation/erosion, time-dependent system porosities, and the three-dimensional geometry of the devices. In contrast with previous theories, this model is able to describe the observed drug release kinetics accurately over the entire period of time, including 1) initial "burst" effects; 2) subsequent, approximately zero-order drug release phases; and 3) second rapid drug release phases. Important information, such as the evolution of the drug concentration profiles within the microparticles, can be calculated. CONCLUSIONS; A new, mechanistic mathematical model was developed that allows further insight into the release mechanisms in bioerodible microparticles.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Siepmann J,Faisant N,Benoit JP

doi

10.1023/a:1021457911533

subject

Has Abstract

pub_date

2002-12-01 00:00:00

pages

1885-93

issue

12

eissn

0724-8741

issn

1573-904X

journal_volume

19

pub_type

杂志文章
  • Poly-L-arginine enhances paracellular permeability via serine/threonine phosphorylation of ZO-1 and tyrosine dephosphorylation of occludin in rabbit nasal epithelium.

    abstract:PURPOSE:The purpose of the present study is to explore whether a poly-L-arginine (poly-L-Arg)-induced increase in tight junctions (TJ) permeability of fluorescein isothiocyanate-labeled dextran (MW 4.4 kDa, FD-4) is associated with the Ca2+-dependent signaling and occurs following the phosphorylation/dephosphorylation ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/b:pham.0000003383.86238.d1

    authors: Ohtake K,Maeno T,Ueda H,Ogihara M,Natsume H,Morimoto Y

    更新日期:2003-11-01 00:00:00

  • Effects of absorption enhancers on human nasal tissue ciliary movement in vitro.

    abstract::Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015872617511

    authors: Hermens WA,Hooymans PM,Verhoef JC,Merkus FW

    更新日期:1990-02-01 00:00:00

  • The glucose-lowering potential of exenatide delivered orally via goblet cell-targeting nanoparticles.

    abstract:PURPOSE:Exenatide, a potent insulinotropic agent, can be used for the treatment of non-insulin-dependent diabetes mellitus. However, the need for frequent injections seriously limits its therapeutic utility. The aim of present report was to develop an orally available exenatide formulation using goblet cell-targeting n...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1513-1

    authors: Li X,Wang C,Liang R,Sun F,Shi Y,Wang A,Liu W,Sun K,Li Y

    更新日期:2015-03-01 00:00:00

  • Purification and partial characterization of an indomethacin hydrolyzing enzyme from pig liver.

    abstract:PURPOSE:Indomethacin is well known to be metabolized via O-demethylation and N-deacylation. In this paper we found an enzyme involved in the hydrolysis of amide-linkage of indomethacin and partially characterized it as well as its substrate specificity. METHODS:An indomethacin hydrolyzing enzyme was purified to homoge...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016061614399

    authors: Terashima K,Takai S,Usami Y,Adachi T,Sugiyama T,Katagiri Y,Hirano K

    更新日期:1996-09-01 00:00:00

  • 16 alpha-hydroxy-(-)-kauranoic acid: a selectively cytotoxic diterpene from Annona bullata.

    abstract::Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16 alpha-hydroxy-(-)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED50 8.25 x 10(-2) micrograms/ml) and selective cytotoxicity against A-5...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015819422479

    authors: Hui YH,Chang CJ,Smith DL,McLaughlin JL

    更新日期:1990-04-01 00:00:00

  • A Microfluidic Diffusion Cell for Fast and Easy Percutaneous Absorption Assays.

    abstract:PURPOSE:Percutaneous absorption assays of molecules for pharmaceutical and cosmetology purposes are important to determine the bioavailability of new compounds, once topically applied. The current method of choice is to measure the rate of diffusion through excised human skin using a diffusion cell. This method however...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1654-x

    authors: Provin C,Nicolas A,Grégoire S,Fujii T

    更新日期:2015-08-01 00:00:00

  • Immobilization of active urokinase on albumin microspheres: use of a chemical dehydrant and process monitoring.

    abstract::A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufac...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015855622459

    authors: Bhargava K,Ando HY

    更新日期:1992-06-01 00:00:00

  • Analysis of the compression mechanics of pharmaceutical agglomerates of different porosity and composition using the Adams and Kawakita equations.

    abstract:PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1007575120817

    authors: Nicklasson F,Alderborn G

    更新日期:2000-08-01 00:00:00

  • A novel topoisomerase II poison GL331 preferentially induces DNA cleavage at (C/G)T sites and can cause telomere DNA damage.

    abstract:PURPOSE:Topoisomerase II (Topo II) preferentially cuts DNA at alternating purine-pyrimidine repeats. Different Topo II poisons may affect Topo II to produce distinct drug-specific DNA cleavage patterns. GL331 is a new podophyllotoxin derivative exhibiting potent Topo II-poisoning activity. Therefore, the sequence selec...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011048831698

    authors: Lee CC,Huang TS

    更新日期:2001-06-01 00:00:00

  • A method to predict the percutaneous permeability of various compounds: shed snake skin as a model membrane.

    abstract::Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015902308676

    authors: Itoh T,Magavi R,Casady RL,Nishihata T,Rytting JH

    更新日期:1990-12-01 00:00:00

  • Characterization of Intestinal and Hepatic CYP3A-Mediated Metabolism of Midazolam in Children Using a Physiological Population Pharmacokinetic Modelling Approach.

    abstract:PURPOSE:Changes in drug absorption and first-pass metabolism have been reported throughout the pediatric age range. Our aim is to characterize both intestinal and hepatic CYP3A-mediated metabolism of midazolam in children in order to predict first-pass and systemic metabolism of CYP3A substrates. METHODS:Pharmacokinet...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2458-6

    authors: Brussee JM,Yu H,Krekels EHJ,Palić S,Brill MJE,Barrett JS,Rostami-Hodjegan A,de Wildt SN,Knibbe CAJ

    更新日期:2018-07-30 00:00:00

  • Determination of free extracellular levels of methotrexate by microdialysis in muscle and solid tumor of the rabbit.

    abstract:PURPOSE:To determine of the pharmacokinetic profile of methotrexate (MTX) in blood and extracellular fluid (ECF) of VX2 tumor and muscle in rabbits. METHODS:Microdialysis probes were inserted into VX2 tumor and in muscle tissue. Following intravenous administration of MTX (30 mg/kg), serial collection of arterial bloo...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011973409022

    authors: Dukic S,Kaltenbach ML,Gourdier B,Marty H,Vistelle R

    更新日期:1998-01-01 00:00:00

  • Local Application of Pyrophosphorylated Simvastatin Prevents Experimental Periodontitis.

    abstract:PURPOSE:Simvastatin (SIM), a HMG-CoA reductase inhibitor widely prescribed for hypercholesterolemia, has been reported to ameliorate inflammation and promote osteogenesis. Its clinical applications on these potential secondary indications, however, have been hampered by its lack of osteotropicity and poor water solubil...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2444-z

    authors: Wang X,Jia Z,Almoshari Y,Lele SM,Reinhardt RA,Wang D

    更新日期:2018-06-25 00:00:00

  • A novel preformulation tool to group microcrystalline celluloses using artificial neural network and data clustering.

    abstract:PURPOSE:To group microcrystalline celluloses (MCCs) using a combination of artificial neural network (ANN) and data clustering. METHODS:Radial basis function (RBF) network was used to model the torque measurements of the various MCCs. Output from the RBF network was used to group the MCCs using a data clustering techn...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-004-7690-6

    authors: Soh JL,Chen F,Liew CV,Shi D,Heng PW

    更新日期:2004-12-01 00:00:00

  • Antibacterial Silver-Conjugated Magnetic Nanoparticles: Design, Synthesis and Bactericidal Effect.

    abstract:PURPOSE:The aim was to design and thoroughly characterize monodisperse Fe3O4@SiO2-Ag nanoparticles with strong antibacterial properties, which makes them a candidate for targeting bacterial infections. METHODS:The monodisperse Fe3O4 nanoparticles were prepared by oleic acid-stabilized thermal decomposition of Fe(III) ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-019-2680-x

    authors: Shatan AB,Venclíková K,Zasońska BA,Patsula V,Pop-Georgievski O,Petrovský E,Horák D

    更新日期:2019-08-14 00:00:00

  • Enhancement of nasal salmon calcitonin absorption by lauroylcarnitine chloride in rats.

    abstract:PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016051600828

    authors: Kagatani S,Shinoda T,Fukui M,Ohmura T,Hasumi S,Sonobe T

    更新日期:1996-05-01 00:00:00

  • Insights into Spray Development from Metered-Dose Inhalers Through Quantitative X-ray Radiography.

    abstract:PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-1869-5

    authors: Mason-Smith N,Duke DJ,Kastengren AL,Stewart PJ,Traini D,Young PM,Chen Y,Lewis DA,Soria J,Edgington-Mitchell D,Honnery D

    更新日期:2016-05-01 00:00:00

  • Development and application of an isolated perfused rat liver model to study the stimulation and inhibition of tumor necrosis factor-alpha production ex vivo.

    abstract:PURPOSE:To develop an isolated perfused rat liver (IPRL) model with low baseline levels of tumor necrosis factor (TNF)-alpha in the outlet perfusate to study the effects of immunostimulants and immunosuppressants on the release of TNF-alpha from this organ. METHODS:Isolated rat livers were perfused with a buffer conta...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1013603331899

    authors: Mehvar R,Zhang X

    更新日期:2002-01-01 00:00:00

  • Synthesis and in vitro evaluation of a novel chitosan-glutathione conjugate.

    abstract:PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-005-6248-6

    authors: Kafedjiiski K,Föger F,Werle M,Bernkop-Schnürch A

    更新日期:2005-09-01 00:00:00

  • Role of Knowledge Management in Development and Lifecycle Management of Biopharmaceuticals.

    abstract::Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-016-2043-9

    authors: Rathore AS,Garcia-Aponte OF,Golabgir A,Vallejo-Diaz BM,Herwig C

    更新日期:2017-02-01 00:00:00

  • Liposomes co-Loaded with 6-Phosphofructo-2-Kinase/Fructose-2, 6-Biphosphatase 3 (PFKFB3) shRNA Plasmid and Docetaxel for the Treatment of non-small Cell Lung Cancer.

    abstract:PURPOSE:Non-small cell lung cancer is the leading cause of cancer related deaths globally. Considering the side effects and diminishing chemosensitivity to chemotherapy, novel treatment approaches are sought. Hence, we aim to develop a liposomal co-delivery system of pDNA expressing shRNA against PFKFB3 (pshPFKFB3) and...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2244-x

    authors: Chowdhury N,Vhora I,Patel K,Doddapaneni R,Mondal A,Singh M

    更新日期:2017-11-01 00:00:00

  • Percolation theory and compactibility of binary powder systems.

    abstract::Defined size fractions of polyethyleneglycol powder (MW = 10,000) were mixed with defined size fractions of alpha-lactose monohydrate in order to study the effect of compaction as a function of the weight ratios of the two excipients. For a precise control of the compression cycle, tablets were compressed on a Univers...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015864415693

    authors: Blattner D,Kolb M,Leuenberger H

    更新日期:1990-02-01 00:00:00

  • Nasal absorption kinetic behavior of azetirelin and its enhancement by acylcarnitines in rats.

    abstract:PURPOSE:The long-term stability and nasal absorption characteristics of a basic nasal formulation of azetirelin, a thyrotropin-releasing hormone analog and its absorption enhancement by incorporation of acylcarnitines in the formulation were investigated. METHODS:The long-term stability of basic nasal azetirelin formu...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011952804479

    authors: Kagatani S,Inaba N,Fukui M,Sonobe T

    更新日期:1998-01-01 00:00:00

  • In vitro/in vivo correlation for 14C-methylated lysozyme release from poly(ether-ester) microspheres.

    abstract:PURPOSE:The purpose of this study was to obtain an in vitro/in vivo correlation for the sustained release of a protein from poly(ethylene glycol) terephthalate (PEGT)/poly(butylene terephthalate) (PBT) microspheres. METHODS:Radiolabeled lysozyme was encapsulated in PEGT/PBT microspheres via a water-in-oil-in-water emu...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/B:PHAM.0000019303.12086.d1

    authors: van Dijkhuizen-Radersma R,Wright SJ,Taylor LM,John BA,de Groot K,Bezemer JM

    更新日期:2004-03-01 00:00:00

  • Structural effects on the binding of amine drugs with the diphenylmethyl functionality to cyclodextrins. I. A microcalorimetric study.

    abstract::Solution calorimetry has been employed to evaluate the stability constants and enthalpy changes associated with complex formation between alpha-, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. Data from thermal titrations of the compounds were analyzed using no...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015880218535

    authors: Tong WQ,Lach JL,Chin TF,Guillory JK

    更新日期:1991-07-01 00:00:00

  • Composite fibrin scaffolds increase mechanical strength and preserve contractility of tissue engineered blood vessels.

    abstract:OBJECTIVES:We recently demonstrated that fibrin-based tissue engineered blood vessels (TEV) exhibited vascular reactivity, matrix remodeling and sufficient strength for implantation into the veins of an ovine animal model, where they remained patent for 15 weeks. Here we present an approach to improve the mechanical pr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-007-9499-6

    authors: Yao L,Liu J,Andreadis ST

    更新日期:2008-05-01 00:00:00

  • Site- and stereospecific ocular drug delivery by sequential enzymatic bioactivation.

    abstract::Intraocular enzymes convert the ketoxime analogues of some beta-adrenergic blockers via a sequential bioactivation process involving hydrolysis to the corresponding ketones followed by reduction to the aryloxyaminoalcohols, which then exert known and predictable physiological and pharmacological effects only at the si...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015863521513

    authors: Bodor N,Prokai L

    更新日期:1990-07-01 00:00:00

  • A spectroscopic investigation of losartan polymorphs.

    abstract::Losartan, an antihypertensive agent in clinical development, was found to exist in two enantiotropic polymorphic forms, a low-temperature stable form (Form I) and a high-temperature stable form (Form II), the temperatures at which they are stable being related to the transition temperature. X-ray powder diffraction pa...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018973530443

    authors: Raghavan K,Dwivedi A,Campbell GC Jr,Johnston E,Levorse D,McCauley J,Hussain M

    更新日期:1993-06-01 00:00:00

  • Nebulization of liposomes. I. Effects of lipid composition.

    abstract::A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 mi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015924124180

    authors: Niven RW,Schreier H

    更新日期:1990-11-01 00:00:00

  • Fatty acid-RGD peptide amphiphile micelles as potential paclitaxel delivery carriers to α(v)β₃ integrin overexpressing tumors.

    abstract:PURPOSE:To design and synthesize fatty acid-RGD peptide amphiphiles with ADA linker for their potential delivery of hydrophobic drugs like paclitaxel targeted to α(v)β(3) integrin overexpressing tumors. METHODS:Four amphiphiles - C16 or C18 fatty acid-RGD peptide and ADA linker were designed and synthesized. CMC, size...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0830-5

    authors: Javali NM,Raj A,Saraf P,Li X,Jasti B

    更新日期:2012-12-01 00:00:00