Protein transduction domain-containing microemulsions as cutaneous delivery systems for an anticancer agent.


:In this study, we developed cationic microemulsions containing a protein transduction domain (penetratin) for optimizing paclitaxel localization within the skin. Microemulsions were prepared by mixing a surfactant blend (BRIJ:ethanol:propylene glycol 2:1:1, w/w/w) with monocaprylin (oil phase) at 1.3:1 ratio, and adding water at 30% (ME-30), 43% (ME-43), and 50% (ME-50). Electrical conductivity and viscosity measurements indicated that ME-30 is most likely a bicontinuous system, whereas ME-43 and ME-50 are water continuous. Their irritation potential, studied in bioengineered skin equivalents, decreased as aqueous content increased. Because ME-50 was not stable in the presence of paclitaxel (0.5%), ME-43 was selected for penetratin incorporation (0.4%). The microemulsion containing penetratin (ME-P) displayed zeta potential of +5.2 mV, and promoted a 1.8-fold increase in paclitaxel cutaneous (but not transdermal) delivery compared with the plain ME-43, whereas the enhancement promoted by another cationic microemulsion containing phytosphingosine was 1.3-fold. Compared with myvacet oil, ME-P promoted a larger increase on transepidermal water loss (twofold) than the plain or the phytosphingosine-containing microemulsions (1.5-fold), suggesting that penetratin addition increases the barrier-disrupting and penetration-enhancing effects of microemulsions. The ratio Δcutaneous/Δtransdermal delivery promoted by ME-P was the highest among the formulations, suggesting its potential for drug localization within cutaneous tumor lesions.


J Pharm Sci


Pepe D,McCall M,Zheng H,Lopes LB




Has Abstract


2013-05-01 00:00:00














  • Partial molal volumes and solubilities of physostigmine in isopropanol:isopropyl myristate solvents in relation to skin penetrability.

    abstract::Partial molal volumes (Vi infinity) of physostigmine, ranging from 232.9 to 239.8 cm3.mol-1, and its mole fraction solubilities (Xi), ranging from 0.051 to 0.009, were determined at 25 degrees C in solutions of isopropanol (IPA), isopropyl myristate (IPM), and their mixtures. An inverse relation was found between Vi i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pardo A,Shiri Y,Cohen S

    更新日期:1991-06-01 00:00:00

  • Effect of powder substrate on foaml drainage and collapse: implications to foam granulation.

    abstract::Foam granulation is a relatively newer wet granulation process whereby foamed binder solutions are added to powders in a mixer. It is essential to understand the effect of powder substrate on foam drainage and half-life, which are relevant to nucleation and agglomeration during foam granulation. Hydroxypropyl methylce...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Koo OM,Ji J,Li J

    更新日期:2012-04-01 00:00:00

  • Pharmacokinetics and tissue distribution after intravenous administration of a single dose of amphotericin B cochleates, a new lipid-based delivery system.

    abstract::Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Segarra I,Movshin DA,Zarif L

    更新日期:2002-08-01 00:00:00

  • Self-setting hydroxyapatite cement: a novel skeletal drug-delivery system for antibiotics.

    abstract::A novel approach using a self-setting hydroxyapatite (HAP) cement as a skeletal drug-delivery system has been proposed to solve the problem of delivering drugs to skeletal tissue at sufficiently high local concentrations for desirable therapeutic effects. HAP cements loaded with antibiotics can be formed in situ and c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yu D,Wong J,Matsuda Y,Fox JL,Higuchi WI,Otsuka M

    更新日期:1992-06-01 00:00:00

  • Effect of characteristics of compounds on maintenance of an amorphous state in solid dispersion with crospovidone.

    abstract::Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms. This study aimed to determine the types of drugs that could adopt a stable amorphous form in SD. Twenty compounds with various melting points (70-218 degrees C), molecular weights (135-504) a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Shibata Y,Fujii M,Kokudai M,Noda S,Okada H,Kondoh M,Watanabe Y

    更新日期:2007-06-01 00:00:00

  • Tripeptide discriminations using circular dichroism detection.

    abstract::A general spectroscopic method is described that might be applied to validating amino acid sequences in peptides and protein fragments with a view to it becoming a routine procedure with which to characterize biotechnology drug products. The tripeptides are the L-enantiomers of GGA, GGH, GGI, GGL, GGF, GHG, LGG, and Y...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Purdie N,Province DW,Johnson EA

    更新日期:1999-07-01 00:00:00

  • Detection of a minor amorphous phase in crystalline etoricoxib by dynamic mechanical analysis: comparison with Raman spectroscopy and modulated differential scanning calorimetry.

    abstract::Detection and quantification of the amorphous phase of etoricoxib bulk drug substances, a selective cycloogenase-2 inhibitor used for the treatment of osteoarthritis, rheumatoid arthritis, and dental pain, was carried out using modulated differential scanning calorimetry (MDSC), dynamic mechanical analysis (DMA), and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Clas SD,Lalonde K,Khougaz K,Dalton CR,Bilbeisi R

    更新日期:2012-02-01 00:00:00

  • Calorimetric determination of the heat of precipitation of pseudoephedrine racemic compound--its agreement with the heat of solution.

    abstract::The heat of precipitation of dl-pseudoephedrine was determined by direct calorimetry using a Tronac isoperibolic calorimeter. The precipitation of dl-pseudoephedrine was induced by mixing aqueous solutions of the two enantiomers, namely, d- and l-pseudoephedrine, directly in the calorimeter. The molar heat of precipit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pudipeddi M,Sokoloski TD,Duddu SP,Carstensen JT

    更新日期:1995-10-01 00:00:00

  • An examination of the thermodynamics of fusion, vaporization, and sublimation of (R,S)- and (R)-flurbiprofen by correlation gas chromatography.

    abstract::The vaporization, fusion, and sublimation enthalpies of (R,S)- and (R)-flurbiprofen at T = 298.15 K are reported and compared with literature values when available. Correlation gas chromatography experiments were first performed to identify appropriate standards that could be used for materials containing a single flu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Umnahanant P,Hasty D,Chickos J

    更新日期:2012-06-01 00:00:00

  • Estimation of the aqueous solubility I: application to organic nonelectrolytes.

    abstract::The estimation of aqueous solubilities of organic nonelectrolytes by the General Solubility Equation (GSE) as proposed by Valvani and Yalkowsky (1980) is used in this study. The data and assumptions on which the GSE are based are reevaluated, and the equation is revised. The revised GSE is validated on a set of 580 ph...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Jain N,Yalkowsky SH

    更新日期:2001-02-01 00:00:00

  • On the mechanism and dynamics of uptake and permeation of polyether-copolyester dendrimers across an in vitro blood-brain barrier model.

    abstract::Dendrimers have emerged as a promising drug delivery system due to their well defined size, tailorability, and multifunctional nature. However, their application in brain delivery is relatively a new area of research. The present study was aimed at evaluating the uptake and permeation of polyether-copolyester (PEPE) d...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Dhanikula RS,Hammady T,Hildgen P

    更新日期:2009-10-01 00:00:00

  • Integrated functions for four basic models of indirect pharmacodynamic response.

    abstract::The integrated solutions (ABEC, area between baseline and effect curve) of four basic models of indirect pharmacodynamic responses are developed. These models assume that drug can inhibit or stimulate the production or loss of the response variable. For two models (I and III) with monoexponential drug disposition, exp...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Krzyzanski W,Jusko WJ

    更新日期:1998-01-01 00:00:00

  • Iontophoretic transdermal delivery of sumatriptan: effect of current density and ionic strength.

    abstract::Iontophoretic transdermal delivery of sumatriptan was investigated in vitro. Among the conditions tested, 0.25 mA/cm2 and low ionic strength (NaCl 25 mM) was the best experimental condition to increase its transport across the skin. The flux increased 385-fold respective to passive diffusion, thus resulting in a trans...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Femenía-Font A,Balaguer-Fernández C,Merino V,López-Castellano A

    更新日期:2005-10-01 00:00:00

  • Oxidation of human insulin-like growth factor I in formulation studies. 3. Factorial experiments of the effects of ferric ions, EDTA, and visible light on methionine oxidation and covalent aggregation in aqueous solution.

    abstract::The influence of ferric ions, EDTA, and visible light on the oxidation of methionine and the covalent reducible and nonreducible dimerization in human Insulin-like Growth Factor I (hIGF-I) in aqueous (1 mM) phosphate buffer solution were studied. A reduced factorial experiment with two levels of each factor was used. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fransson JR

    更新日期:1997-09-01 00:00:00

  • Delivery of the photosensitizer Pc 4 in PEG-PCL micelles for in vitro PDT studies.

    abstract::The silicon phthalocyanine Pc 4 is a second-generation photosensitizer that has several properties superior to other photosensitizers currently approved by the FDA, and it has shown significant promise for photodynamic therapy (PDT) in several cancer cells in vitro and model tumor systems in vivo. However, because of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Master AM,Rodriguez ME,Kenney ME,Oleinick NL,Gupta AS

    更新日期:2010-05-01 00:00:00

  • A system approach to pharmacodynamics. Input-effect control system analysis of central nervous system effect of alfentanil.

    abstract::Virtually all biological variables, including those affected by drugs, are subject to adaptive self regulation. In the description of the pharmacodynamics (PD) of drugs, it may be necessary to consider the endogenous control system (ECS) as an integral part of the PD. A PDECS model based on system analysis principles ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Veng-Pedersen P,Modi NB

    更新日期:1993-03-01 00:00:00

  • Cobaltous choride-induced hypothermia in mice I: effect of pretreatment with anticholinergic drugs.

    abstract::The hypothermic response following intraperitoneal doses (6.25, 12.5, and 25 mg/kg) of cobaltous chloride was investigated in Swiss albino mice. The magnitude and duration of rectal temperature depression were dose related. In each case, maximal hypothermia was evident within 30 min after injection. Body temperature d...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Burke DH

    更新日期:1978-06-01 00:00:00

  • In situ perfusion system for oral mucosal absorption in dogs.

    abstract::To evaluate oral mucosal absorption of drugs in dogs, a newly designed in situ perfusion system with a circulating perfusion chamber was developed. The utility of the perfusion system was investigated by using three drugs: salicylic acid (SA), sulfadimethoxine (SM), and diltiazem (DIL). The oral mucosal absorption of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yamahara H,Suzuki T,Mizobe M,Noda K,Samejima M

    更新日期:1990-11-01 00:00:00

  • Stability of aqueous solutions of pirbuterol.

    abstract::The hydrolytic degradation of pirbuterol was investigated under saturated oxygen conditions over a wide range of pH values and at different temperatures. Two of the five observed breakdown products were positively identified. The first-order decomposition rate appeared to depend on the rate constants of the four disso...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bansal PC,Monkhouse DC

    更新日期:1977-06-01 00:00:00

  • Hot Melt Extrusion as Solvent-Free Technique for a Continuous Manufacturing of Drug-Loaded Mesoporous Silica.

    abstract::The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Genina N,Hadi B,Löbmann K

    更新日期:2018-01-01 00:00:00

  • Nasal drug administration: potential for targeted central nervous system delivery.

    abstract::Nasal administration as a means of delivering therapeutic agents preferentially to the brain has gained significant recent interest. While some substrates appear to be delivered directly to the brain via this route, the mechanisms governing overall brain uptake and exposure remain unclear. Some substrates utilize the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Graff CL,Pollack GM

    更新日期:2005-06-01 00:00:00

  • Finding the Needle in the Haystack: High-Resolution Techniques for Characterization of Mixed Protein Particles Containing Shed Silicone Rubber Particles Generated During Pumping.

    abstract::During the manufacturing process of biopharmaceuticals, peristaltic pumps are employed at different stages for transferring and dosing of the final product. Commonly used silicone tubings are known for particle shedding from the inner tubing surface due to friction in the pump head. These nanometer sized silicone rubb...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Deiringer N,Haase C,Wieland K,Zahler S,Haisch C,Friess W

    更新日期:2020-12-09 00:00:00

  • Hydrogen-bonded complexes between chloral hydrate and halide ions in aqueous solution.

    abstract::The hydrogen-bonded interactions of chloral hydrate and halide ions have been investigated conductometrically at 25.00 degrees C in aqueous solutions. In spite of the strong competing effect of water, the 1:1 associates have relatively high stability constants, in the order of chloride greater than bromide greater tha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Barcza L,Lenner L

    更新日期:1988-07-01 00:00:00

  • Physical stability comparisons of IgG1-Fc variants: effects of N-glycosylation site occupancy and Asp/Gln residues at site Asn 297.

    abstract::The structural integrity and conformational stability of various IgG1-Fc proteins produced from the yeast Pichia pastoris with different glycosylation site occupancy (di-, mono-, and nonglycosylated) were determined. In addition, the physical stability profiles of three different forms of nonglycosylated Fc molecules ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Alsenaidy MA,Okbazghi SZ,Kim JH,Joshi SB,Middaugh CR,Tolbert TJ,Volkin DB

    更新日期:2014-06-01 00:00:00

  • Evaluation of 6β-Hydroxycortisol and 6β-Hydroxycortisone as Biomarkers for Cytochrome P450 3A Activity: Insight into Their Predictive Value for Estimating Oral Immunosuppressant Metabolism.

    abstract::The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

    更新日期:2015-10-01 00:00:00

  • Synthesis and biological investigations of some 5H-1,3,4-oxadiazolo[3,2-a]pyrimidin-5-ones.

    abstract::The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Soliman FS,Shafik RM,Darwish M

    更新日期:1982-02-01 00:00:00

  • Targeted Drug Delivery via Folate Receptors for the Treatment of Brain Cancer: Can the Promise Deliver?

    abstract::Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Guo J,Schlich M,Cryan JF,O'Driscoll CM

    更新日期:2017-12-01 00:00:00

  • Implementation of an ADME enabling selection and visualization tool for drug discovery.

    abstract::The pharmaceutical industry has large investments in compound library enrichment, high throughput biological screening, and biopharmaceutical (ADME) screening. As the number of compounds submitted for in vitro ADME screens increases, data analysis, interpretation, and reporting will become rate limiting in providing A...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Stoner CL,Gifford E,Stankovic C,Lepsy CS,Brodfuehrer J,Prasad JV,Surendran N

    更新日期:2004-05-01 00:00:00

  • A physiologically based pharmacokinetic model of zidovudine (AZT) in the mouse: model development and scale-up to humans.

    abstract::After having been used in treating HIV infection for a decade, zidovudine (AZT) continues to be an essential component of antiretroviral regimens. Because antiviral responses and toxicity of AZT seem to be related to cells in specific target tissues, being able to understand and predict the distribution of AZT into di...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chow HH

    更新日期:1997-11-01 00:00:00

  • Video characterization of flume patterns of inhalation aerosols.

    abstract::An in vitro technique was developed to characterize the intermittent flume patterns associated with the short bursts of metered-dose aerosols. Two orthogonal video images are utilized to describe the complex shape and direction of the flume pattern. This technique facilitates the evaluation of components manufactured ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Miszuk S,Gupta BM,Chen FC,Clawans C,Knapp JZ

    更新日期:1980-06-01 00:00:00