Abstract:
:Microporous polymeric matrices prepared from poly(ɛ-caprolactone) [PCL] were evaluated for controlled vaginal delivery of the antiprotozoal agent (tinidazole) in the treatment of the sexually transmitted infection, trichomoniasis. The matrices were produced by rapidly cooling co-solutions of PCL and tinidazole in acetone to -80 °C to induce crystallisation and hardening of the polymer. Tinidazole incorporation in the matrices increased from 1.4 to 3.9% (w/w), when the drug concentration in the starting PCL solution was raised from 10 to 20% (w/w), giving rise to drug loading efficiencies up to 20%. Rapid 'burst release' of 30% of the tinidazole content was recorded over 24 h when the PCL matrices were immersed in simulated vaginal fluid. Gradual drug release occurred over the next 6 days resulting in delivery of around 50% of the tinidazole load by day 7 with the released drug retaining antiprotozoal activity at levels almost 50% that of the 'non-formulated' drug in solution form. Basic modelling predicted that the concentration of tinidazole released into vaginal fluid in vivo from a PCL matrix in the form of an intravaginal ring would exceed the minimum inhibitory concentration against Trichomonas vaginalis. These findings recommend further investigation of PCL matrices as intravaginal devices for controlled delivery of antiprotozoal agents in the treatment and prevention of sexually transmitted infections.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Fernando HV,Chan LL,Dang N,Santhanes D,Banneheke H,Nalliah S,Coombes AGAdoi
10.1080/10837450.2018.1481430subject
Has Abstractpub_date
2019-03-01 00:00:00pages
348-356issue
3eissn
1083-7450issn
1097-9867journal_volume
24pub_type
杂志文章abstract::Submicron colloidal suspensions of poly(epsilon-caprolactone) (PCL) were prepared by the solvent displacement method, using either the conventional form or a new recirculation device. In the latter case, a process that allows the recirculation of the aqueous phase into a device, providing a continuous flow, is propose...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450600940824
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abstract::The compendial method of evaluation of orodispersible tablets (ODT) is the same disintegration test as for conventional tablets. Since it does not reflect the disintegration process in the oral cavity, alternative methods are proposed that are more related to in vivo conditions, e.g. modified dissolution paddle appara...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2012.710238
更新日期:2013-03-01 00:00:00
abstract::An osmotic-controlled pulsatile delivery technology was developed for targeted drug delivery. This novel system consists of a tablet core surrounded by an osmotic coating that has been mechanically compromised in strategic locations to facilitate reliable drug release at a given time point after administration. The ta...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450902838692
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abstract::The objectives of this research were to evaluate the stability of lercanidipine in solution state and solid state and explore the compatibility of drug with oils, surfactants and cosurfactants as excipients. The effect of pH on the degradation in solution state was studied through pH-rate profile of lercanidipine in c...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2011.580758
更新日期:2012-11-01 00:00:00
abstract::The purpose of this work was to prepare and characterize Angiopep-2 functionalized ginsenoside-Rg3 loaded nanoparticles (ANG-Rg3-NP) and evaluate the therapeutic effect on C6 glioma cells. Nanoparticles were prepared by the emulsion solvent evaporation method. Angiopep-2 was functionalized to nanoparticles via a malei...
journal_title:Pharmaceutical development and technology
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abstract:PURPOSE:The purpose of this study is to investigate the mechanisms and thermodynamics of the interaction between hydroxypropyl beta-cyclodextrin (HPdetaCD) and [D-Trp6, des-Gly10] LHRH ethylamide (deslorelin), a peptide drug. METHODS:We used UV and fluorescence spectroscopy to study the interaction of HPbetaCD and des...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120000297
更新日期:2001-11-01 00:00:00
abstract::The aim of this study was to investigate early formulation screening in small scale with a miniaturized fluid bed device. Altogether eight different batches were granulated in a Multipart Microscale Fluid bed Powder processor (MMFP) with constant process conditions using electrostatic atomization. Atomization voltage ...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837451003739271
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abstract::The purpose of this study was to investigate the effect of the composition of a binary powder mixture on the bonding index, the brittle fracture index, and the strain index, as defined by Hiestand. The studies involved tensile strength and dynamic indentation hardness determinations of square compacts, the solid fract...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837459709022630
更新日期:1997-11-01 00:00:00
abstract::Drug-excipient compatibility studies lay the foundation for designing a chemically stable formulation for clinical and commercial development. This article describes the investigation of oxidative degradation encountered with compound A (a phenylalanine-drug complex) in a capsule dosage form. Two wet- granulation caps...
journal_title:Pharmaceutical development and technology
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abstract::A novel analytical procedure has been developed for quantitative determination of levodopa and carbidopa in aqueous binary solutions acidified by HCl and without any other sample pretreatment. The method is based partially on least squares treatment of data obtained by attenuated total reflectance Fourier transform in...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450701481249
更新日期:2007-01-01 00:00:00
abstract::This work aimed to incorporate Dexibuprofen (DXI), the pharmacologically active and more potent form of ibuprofen, into polymeric micelles based tablets with enhanced oral bioavailability. Thin film hydration technique was employed to prepare DXI polymeric micelles using Pluronic® F127 and/or P123 solutions in differe...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2013.823994
更新日期:2014-09-01 00:00:00
abstract::Letrozole (LTZ), an aromatase inhibitor used for the treatment of hormonally-positive breast cancer in postmenopausal women, has poor water solubility, rapid metabolism, and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been designed and characterized, aimed to c...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450.2018.1455698
更新日期:2019-02-01 00:00:00
abstract::The formulation of betamethasone-17-valerate (BV) into topical medicines presents a significant challenge for the formulation chemist. The substance is susceptible to acid and base catalyzed isomerization in aqueous environments, which results in valerate transesterification from carbon 17 to carbon 21 of the steroid ...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2016.1143003
更新日期:2017-06-01 00:00:00
abstract::Transdermal drug administration has a number of advantages that cannot be leveraged for therapeutic benefits because of the robust barrier provided by the stratum corneum. One of the promising techniques for circumventing the stratum corneum is sonophoresis - the use of ultrasound for facilitating transdermal drug del...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章,评审
doi:10.3109/10837450.2015.1116566
更新日期:2017-06-01 00:00:00
abstract::The physical stability of amorphous solid dispersions (SDs) is influenced by their storage conditions. The goal of this work was to investigate the factors affecting the recrystallization of drugs in SDs after storage under conditions of high temperature and high humidity. SDs of three drugs (dipyridamole, nifedipine ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2013.795168
更新日期:2014-06-01 00:00:00
abstract::Elderly people, children and patients sometimes have difficulties swallowing tablets. To solve this problem, a novel method of preparing tablets that disintegrate rapidly in the mouth was developed. A tablet with high porosity is required for rapid disintegration, but such a tablet is generally fragile. To make a tabl...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120000287
更新日期:2001-11-01 00:00:00
abstract:PURPOSE:BMS-196843 (Oncostatin M) is a therapeutic recombinant protein in development. Scale-up process changes led to unexpected instability of the bulk drug substance solution during storage. A product with an apparent higher MW than the parent protein was observed by the size-exclusion chromatography (SEC). This stu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100002202
更新日期:2001-01-01 00:00:00
abstract::Vardenafil hydrochloride (VAR) is an erectile dysfunction treating drug. VAR has a short elimination half-life (4-5 h) and suffers low oral bioavailability (15%). This work aimed to explore the dual potential of VAR-dendrimer complexes as drug release modulators and oral bioavailability enhancers. VAR-dendrimer comple...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450.2018.1472611
更新日期:2019-03-01 00:00:00
abstract::The purpose of this study was to develop a method to prepare Metoprolol Succinate (MS) sustained release pellets and compress them into pellet-containing tablets without losing sustained release property. The drug layered pellets were coated with Eudragit NE 30D to obtain a sustained release (SR) property. The mechani...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1081612
更新日期:2016-12-01 00:00:00
abstract::The present study was aimed to develop a matrix-type transdermal formulation of pentazocine using mixed polymeric grades of Eudragit RL/RS. The possible interaction between drug and polymer used were characterized by FTIR, DSC and X-RD. X-RD study indicates a change of state of drug from crystalline to amorphous in th...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450903188501
更新日期:2010-06-01 00:00:00
abstract::The effect of some processing and formulation variables on the stability of tablets containing a crystalline salt of a triazine derivative was studied. The salt has a relatively low melting point and a low microenvironmental pH due to the weakly basic nature of the parent compound (pKa = 4.0). This compound decomposes...
journal_title:Pharmaceutical development and technology
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doi:10.1081/pdt-200031417
更新日期:2004-08-01 00:00:00
abstract::The use of rice bran (RB), soybean (SB) or sunflower seed (SF) oils to prepare lipid-core nanocapsules (LNCs) as controlled drug delivery systems was investigated. LNCs were prepared by interfacial deposition using the preformed polymer method. All formulations showed negative zeta potential and adequate nanotechnolog...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2013.829097
更新日期:2014-11-01 00:00:00
abstract::Flecainide base is pharmaceutically active substance used for production of flecainide acetate which is known in market as Tambacor, Almarytm, Apocard, Ecrinal or Flecaine. It is determined that flecainide base forms four polymorphic forms abbreviated as Ib, IIb, IIIb and IVb. Flecainide base form Ib is thermodynamica...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2013.763259
更新日期:2014-02-01 00:00:00
abstract::The purpose of this paper was to investigate the effect of several experimental variables on the ability of a neural network to predict in vitro dissolution rate as a function of product formulation changes. Neural network software was trained with sets of hypothetical and experimental data consisting of 4-15 formulat...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459709031442
更新日期:1997-08-01 00:00:00
abstract::Two types of casein hydrolysates, casein A (mean peptide length 3.3) and casein B (mean peptide length 17.4) were prepared by the enzymatic hydrolysis of casein, and their effects on in vitro dissolution rates and oral bioavailability of drugs were evaluated. The in vitro dissolution behavior of the kneaded mixture of...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809028499
更新日期:1998-05-01 00:00:00
abstract::Two polymorphs and three solvates of fluconazole were isolated and characterized by x-ray powder diffractometry, IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetry, and their dissolution rates. The different forms were prepared by crystallization of the original powder in different solvents at ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120015052
更新日期:2002-11-01 00:00:00
abstract::The unstirred aqueous boundary layer (ABL) thickness was determined for modified Franz diffusion cells using three test compounds--parathion, 4-hexylresorcinol, and 2,4-dinitrochlorobenzene (DNCB). Steady-state fluxes through one, two, and three dialysis membranes in series were achieved in donor-saturated, infinite-d...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.572895
更新日期:2012-11-01 00:00:00
abstract::Microgels were prepared by cinnamic acid-gelatin (type B) conjugate (CA-GelB) and cinnamic acid-Pluronic F127 conjugate (CA-Plur). (1)H NMR confirmed that CA was conjugated to gelatin and the gelatin to CA residue molar ratio was estimated to be 1:4.7 by a colorimetric method. CA-Plur of which the CA residue to Plur m...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.999787
更新日期:2016-01-01 00:00:00
abstract::Ternary complexes of meloxicam (ML), a poorly water-soluble anti-inflammatory drug, with β-cyclodextrin (βCD) and polyethylene glycol (PEG) 6000 were prepared from an equimolar (ML-βCD) and 10% of PEG. Characterization of the ternary complex was carried out by differential scanning calorimetry and X-ray diffractometry...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.565347
更新日期:2012-09-01 00:00:00
abstract:PURPOSE:To investigate the influence of the pH of the dissolution medium on immediate release 850 mg metformin hydrochloride tablets. METHODS:A traditional wet granulation method was used to manufacture metformin hydrochloride tablets with or without a disintegrant. Tablet dissolution was conducted using the USP appar...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.892132
更新日期:2015-01-01 00:00:00