Preparation, preliminary pharmacokinetics and brain tissue distribution of Tanshinone IIA and Tetramethylpyrazine composite nanoemulsions.

Abstract:

:Objective: Tanshinone IIA (TSN) and Tetramethylpyrazine (TMP) were combined in a composite, oil-in-water nanoemulsions (TSN/TMP O/W NEs) was prepared to prolong in vitro and vivo circulation time, and enhance the bioavailability of TSN. Material and methods: Physicochemical characterization of TSN/TMP O/W NEs was characterized systematically. The in vitro dissolution and in vivo pharmacokinetic experiments of TSN/TMP O/W NEs were also evaluated. Result: A formulation was optimized, yielding a 32.5 nm average particle size, an encapsulation efficiency of over 95 %, and were spherical in shape as shown by TEM. TSN/TMP O/W NEs were shown to extend the release and availability in vitro compared to raw compounds. In pharmacokinetic study, the AUC0→∞ and t1/2 of the TSN/TMP O/W NEs were 481.50 mg/L*min and 346.39 min higher than TSN solution, respectively. Brain tissue concentration of TSN was enhanced with TSN/TMP O/W NEs over raw TSN and even TSN O/W NEs. Conclusions: Therefore, nanoemulsions are an effective carrier to increase encapsulation efficiency of drugs, improve bioavailability and brain penetration for TSN - which is further enhanced by pairing with the co-delivery of TMP, providing a promising drug delivery.

journal_name

Pharm Dev Technol

authors

Wang B,Hong L,Liu Y,Bedingfield SK,Zhang C,Peng C,Qian J,Zha L

doi

10.1080/10837450.2019.1656237

subject

Has Abstract

pub_date

2019-12-01 00:00:00

pages

1236-1242

issue

10

eissn

1083-7450

issn

1097-9867

journal_volume

24

pub_type

杂志文章
  • Formulation design, challenges, and development considerations for fixed dose combination (FDC) of oral solid dosage forms.

    abstract::Fixed dose combination (FDC) products are common in the treatment of hypertension, diabetes, human immunodeficiency virus, and tuberculosis. They make it possible to combine two or more drug molecules with different modes of pharmacological actions in a single dosing unit and optimize the treatment. From a patient per...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章,评审

    doi:10.3109/10837450.2012.660699

    authors: Desai D,Wang J,Wen H,Li X,Timmins P

    更新日期:2013-11-01 00:00:00

  • Formulation and processing factors influencing the adhesion of film coats to tablet cores.

    abstract::The effect of six factors: spray gun, formulation, inlet temperature, atomizing air pressure, fan air pressure, and gun-bed distance, on the final adhesion of the film coat to the tablet core were assessed. The method used was based on an experimental design, Resolution IV, that allowed the main effects to be free fro...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-49692

    authors: Khan H,Fell JT,Macleod GS

    更新日期:2005-01-01 00:00:00

  • Physiological parameters of the gastrointestinal fluid impact the dissolution behavior of the BCS class IIa drug valsartan.

    abstract::The objective of this study was to investigate the effect of the physiological parameters (pH, buffer capacity, and ionic strength) of the gastrointestinal (GI) fluid on the dissolution behavior of the class II weakly acidic (BCS class IIa) drug valsartan. A series of in vitro dissolution studies was carried out on Di...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1536996

    authors: Hamed R

    更新日期:2018-12-01 00:00:00

  • Preparation and in vitro characterization of diltiazem hydrochloride loaded alginate microspheres.

    abstract::The main objective of the present study was to improve bioavailability of diltiazem hydrochloride and decrease the frequency of dosage form administration by increasing the encapsulation efficiency of the drug, residence time of the dosage form at the site of absorption and sustained release of the drug from the deliv...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802626304

    authors: Sultana Y,Mall S,Maurya DP,Kumar D,Das M

    更新日期:2009-01-01 00:00:00

  • Formulation strategy of nitrofurantoin: co-crystal or solid dispersion?

    abstract::Poor solubility and bioavailability of drugs are often affected by its microscopic structural properties. Nitrofurantoin (NF), a Biopharmaceutics Classification System class II item, has a low water solubility with low plasma concentrations. To improve its therapeutic efficacy, formulation strategy of solid dispersion...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1689401

    authors: Teoh XY,Bt Mahyuddin FN,Ahmad W,Chan SY

    更新日期:2020-02-01 00:00:00

  • Preparation and characterization of letrozole-loaded poly(d,l-lactide) nanoparticles for drug delivery in breast cancer therapy.

    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

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1455698

    authors: Alemrayat B,Elhissi A,Younes HM

    更新日期:2019-02-01 00:00:00

  • A method for the preparation of sustained release-coated Metoprolol Succinate pellet-containing tablets.

    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

    authors: Yang Z,Yu J,Yang T,Xing H,Zhang J,Xian L,Ding P,Wang D

    更新日期:2016-12-01 00:00:00

  • Co-solvent solubilization of some poorly-soluble antidiabetic drugs.

    abstract::Co-solvent solubilization approach has been used to enhance the solubility of seven antidiabetic drugs: gliclazide, glyburide, glipizide, glimepiride, repaglinide, pioglitazone, and roziglitazone. Solubility in water, phosphate buffer (pH 7.4), six co-solvent solutions prepared in water as well as phosphate buffer (pH...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802498894

    authors: Seedher N,Kanojia M

    更新日期:2009-01-01 00:00:00

  • Stability of dry coated solid dosage forms.

    abstract::The dry coating process was evaluated in terms of storage stability investigating drug release and agglomeration tendency of the different coated oral dosage forms; hydroxypropyl methylcellulose acetate succinate (HPMCAS) was used with triethylcitrate (TEC) as plasticizer and acetylated monoglyceride (Myvacet) as wett...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450902882336

    authors: Kablitz CD,Urbanetz NA

    更新日期:2009-01-01 00:00:00

  • Formulation, development, and in-vitro/ex-vivo evaluation of vaginal bioadhesive salbutamol sulfate tablets for preterm labor.

    abstract::Preterm labor is the main cause of death and serious illness of both infants and pregnant women in Africa and worldwide. Parenteral and oral salbutamol sulfate as a B2 antagonist has been used for the treatment of preterm labor. The study aims are to formulate salbutamol sulfate non-invasive vaginal bioadhesive tablet...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1767129

    authors: El-Enin ASMA,Elbakry AM,Hosary RE,Lotfy MAF

    更新日期:2020-10-01 00:00:00

  • Effects of light intensity, n-alcohols, water-soluble colorants, and solution viscosity on photoisomerization of sorivudine.

    abstract::Effects of various factors, such as light intensity, polarizability of n-alcohol solvents, addition of colorants, and viscosity of solutions on the kinetics of the photoisomerization of therapeutically effective E-isomer of sorivudine to its less effective Z-isomer were studied. Solutions of known concentrations of E-...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100000047

    authors: Desai D,Li D,Janjikhel R,Lang B,Jain N

    更新日期:2001-01-01 00:00:00

  • About the equivalence between different batches of a glycopeptide drug.

    abstract:CONTEXT:Teicoplanin is a glycopeptide antibiotic consisting of a combination of different active components. Clinical equivalence between different batches of this drug is not guaranteed by the present pharmacopeial specification of chemical composition based on an HPLC chromatogram. OBJECTIVE:To test a modification o...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1035726

    authors: Boix-Montañes A,Garcia-Arieta A

    更新日期:2016-08-01 00:00:00

  • Development and evaluation of a laboratory-scale apparatus to simulate the scale-up of a sterile semisolid and effects of manufacturing parameters on product viscosity.

    abstract::The purpose of this study was to develop a benchtop apparatus to simulate the scale-up of the moist-heat sterilization process of sodium carboxymethylcellulose (CMC) gel and identify critical process parameters that affect the sterilized gel viscosity. A 600-ml benchtop Parr reactor was modified and used to achieve go...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100101394

    authors: Chu PI,Doyle D

    更新日期:1999-01-01 00:00:00

  • Preparation and optimization of glyceryl behenate-based highly porous pellets containing cilostazol.

    abstract::The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion/spheronization and sublimation under vacuum. Granules p...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2016.1245743

    authors: Hwang KM,Byun W,Cho CH,Park ES

    更新日期:2018-06-01 00:00:00

  • Gas-saturated solution process to obtain microcomposite particles of alpha lipoic acid/hydrogenated colza oil in supercritical carbon dioxide.

    abstract::Alpha lipoic acid (ALA), an active substance in anti-aging products and dietary supplements, need to be masked with an edible polymer to obscure its unpleasant taste. However, the high viscosity of the ALA molecules prevents them from forming microcomposites with masking materials even in supercritical carbon dioxide ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1049707

    authors: Mishima K,Honjo M,Sharmin T,Ito S,Kawakami R,Kato T,Misumi M,Suetsugu T,Orii H,Kawano H,Irie K,Sano K,Mishima K,Harada T,Ouchi M

    更新日期:2016-09-01 00:00:00

  • Pharmacokinetics of 16-dehydropregnenolone hydroxypropyl-β-cyclodextrin inclusion complex following peroral administration.

    abstract::16-Dehydropregnenolone (16-DHP) is an active compound with an unsatisfied in vivo behavior and poor water-solubility, which limits its clinical application. To improve its in vivo behavior and water-solubility, a Hydroxypropyl-beta-Cyclodextrin (HP-β-CD) inclusion complex of 16-DHP was prepared in this paper. Pharmaco...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2016.1193192

    authors: Sun Y,Jia L,Zhou H,Mao M,Wang X,Wei L,Sun L

    更新日期:2017-03-01 00:00:00

  • Understanding drug-excipient compatibility: oxidation of compound A in a solid dosage form.

    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

    pub_type: 杂志文章

    doi:10.1080/10837450903182140

    authors: Wu Y,Dali M,Gupta A,Raghavan K

    更新日期:2009-01-01 00:00:00

  • Polymorphism and solvates of flecainide base.

    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

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.763259

    authors: Veldre K,Eglīte Z,Actiņš A,Zvirgzdiņš A,Rozenberga L,Tamanis E

    更新日期:2014-02-01 00:00:00

  • Phase transition of a microemulsion upon addition of cyclodextrin - applications in drug delivery.

    abstract::This study reports on the impact of cyclodextrin addition on the phase behavior of microemulsion systems. Three distinct oil-in-water microemulsions were formulated and subjected to increasing concentrations of various cyclodextrins. The prepared formulations underwent visual, textural and microscopic characterization...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1371191

    authors: Thakur SS,Solloway J,Stikkelman A,Seyfoddin A,Rupenthal ID

    更新日期:2018-02-01 00:00:00

  • Eudragit-based transdermal delivery system of pentazocine: Physico-chemical, in vitro and in vivo evaluations.

    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

    pub_type: 杂志文章

    doi:10.3109/10837450903188501

    authors: Chandak AR,Prasad Verma PR

    更新日期:2010-06-01 00:00:00

  • Taste masking of Etoricoxib by using ion-exchange resin.

    abstract::The present study was carried out in order to mask the bitter taste of the Etoricoxib by complexation with cation-exchange resin, Indion 204. The drug resin complexes (DRC) were prepared by batch process and efficient drug loading was obtained by using inactivated form of resin in the drug-resin ratio 1:3.3 with 30 mi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903322787

    authors: Patra S,Samantaray R,Pattnaik S,Barik BB

    更新日期:2010-09-01 00:00:00

  • One-step preparation of ibuprofen fast- and sustained-release formulation by electrospinning with improved efficacy and reduced side effect.

    abstract::In this study, we developed a one-step method to prepare ibuprofen fast- and sustained-release complex preparation. It was based on a double jets electrospinning process. Ibuprofen, a poorly water-soluble drug, was electrospun into fibers with polyvinyl pyrrolidone and hydroxypropyl methyl cellulose by two jets, respe...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1728773

    authors: Che X,Xue J,Zhang J,Yang X,Wang L

    更新日期:2020-07-01 00:00:00

  • Preparation of a reproducible long-acting formulation of risperidone-loaded PLGA microspheres using microfluidic method.

    abstract::The aim of the present study is to prepare risperidone-loaded poly lactic-co-glycolic acid (PLGA) microspheres within microfluidic system and to achieve a formulation with uniform size and monotonic and reproducible release profile. In comparison to batch method, T-junction and serpentine chips were utilized and optim...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2016.1221426

    authors: Jafarifar E,Hajialyani M,Akbari M,Rahimi M,Shokoohinia Y,Fattahi A

    更新日期:2017-09-01 00:00:00

  • Development of controlled-release SK&F 82526-J buffer bead formulations with tartaric acid as the buffer.

    abstract::The purpose of this research was to design and develop a novel controlled-release bead formulation for oral administration with buffer crystals as a carrier for loading of fenoldopam mesylate, an intravenous antihypertensive agent, which provides an in vitro release rate of 30-50 mg/hr for 6-8 hr. Buffer crystals were...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459809028629

    authors: Venkatesh GM

    更新日期:1998-11-01 00:00:00

  • Design and evaluation of ocular drug delivery system for controlled delivery of gatifloxacin sesquehydrate: In vitro and in vivo evaluation.

    abstract::The objective of this investigation was to formulate ocular inserts of gatifloxacin sesquehydrate to achieve controlled drug release. Drug reservoir was prepared using hydrophilic polymers, namely polyvinyl alcohol and polyvinyl pyrrolidone. The rate controlling membrane was prepared using hydrophobic ethyl cellulose ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.502178

    authors: Patel UL,Chotai NP,Nagda CD

    更新日期:2012-01-01 00:00:00

  • Formulation and evaluation of curcumin gel for topical application.

    abstract::The aim of the present investigation was to develop and study topical gel delivery of curcumin for its anti-inflammatory effects. Carbopol 934P (CRB) and hydroxypropylcellulose (HPC) were used for the preparation of gels. The penetration enhancing effect of menthol (0-12.5% w/w) on the percutaneous flux of curcumin th...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802409438

    authors: Patel NA,Patel NJ,Patel RP

    更新日期:2009-01-01 00:00:00

  • A novel approach to increase oral drug absorption.

    abstract::A comprehensive analytical solution that accounts for many factors and assumptions affecting drug concentration profile in the gastrointestinal tract was presented. A sensitivity analysis approach was utilized in order to investigate the importance of different parameters in the model. The partition coefficient is fou...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100000741

    authors: Idkaidek NM,Abdel-Jabbar N

    更新日期:2001-01-01 00:00:00

  • Effect of storage conditions on the recrystallization of drugs in solid dispersions with crospovidone.

    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

    authors: Shibata Y,Fujii M,Suzuki A,Koizumi N,Kanada K,Yamada M,Watanabe Y

    更新日期:2014-06-01 00:00:00

  • Multiunit controlled-release diclofenac sodium capsules using complex of chitosan with sodium alginate or pectin.

    abstract::This study explored the application of chitosan-alginate (CA) and chitosan-pectin (CP) complex films as drug release regulator for the preparation of multiunit controlled-release diclofenac sodium capsules. Pellets containing drug and microcrystalline cellulose, in a ratio of 3:5, were prepared in a fluidized rotary g...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100002247

    authors: Mitrevej A,Sinchaipanid N,Rungvejhavuttivittaya Y,Kositchaiyong V

    更新日期:2001-08-01 00:00:00

  • Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line.

    abstract::The aim of this work is development of a nontoxic, long-term stable solid lipid nanoparticles (SLN) formulation for the loading of Nimesulide (NiM) by a 22 factorial design. The optimized formulation was composed of 10 wt% of glyceryl behenate and 2.5 wt% of poloxamer 188. Immediately after production, Z-Ave of NiM-SL...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1549075

    authors: Campos JR,Fernandes AR,Sousa R,Fangueiro JF,Boonme P,Garcia ML,Silva AM,Naveros BC,Souto EB

    更新日期:2019-06-01 00:00:00