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

Abstract:

: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.

journal_name

J Pharm Sci

authors

Pepe D,McCall M,Zheng H,Lopes LB

doi

10.1002/jps.23482

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

1476-87

issue

5

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)31107-2

journal_volume

102

pub_type

杂志文章
  • In vitro iontophoretic studies using a synthetic membrane.

    abstract::In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780308

    authors: Tu YH,Allen LV Jr

    更新日期:1989-03-01 00:00:00

  • Zidovudine transport in the rabbit brain during intravenous and intracerebroventricular infusion.

    abstract::The distribution of zidovudine (AZT) between plasma, brain extracellular fluid (ECF), and cerebrospinal fluid (CSF) was investigated in a crossover design study (n = 5) in unanesthetized rabbits. Drug was administered by intravenous (iv) and intracerebroventricular (icv) infusions at the same infusion rate (1.5 mg/h.k...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840717

    authors: Wang Y,Sawchuk RJ

    更新日期:1995-07-01 00:00:00

  • Bioavailability and efficacy of antisense morpholino oligomers targeted to c-myc and cytochrome P-450 3A2 following oral administration in rats.

    abstract::Antisense phosphorodiamidate Morpholino oligomers (PMO) are resistant to degradation by cellular hydrolases, DNases, RNases, and phosphodiesterases, but remain sensitive to prolonged exposure to low pH. The present studies evaluate the oral fractional bioavailability, stability, and efficacy of two distinct PMO sequen...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10088

    authors: Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

    更新日期:2002-04-01 00:00:00

  • Drug release from hydrophilic matrices. 2. A mathematical model based on the polymer disentanglement concentration and the diffusion layer.

    abstract::A comprehensive model is developed to describe the swelling/dissolution behaviors and drug release from hydrophilic matrices. The major thrust of this model is to employ an important physical property of the polymer, the polymer disentanglement concentration, rho p,dis, the polymer concentration below which polymer ch...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600841214

    authors: Ju RT,Nixon PR,Patel MV,Tong DM

    更新日期:1995-12-01 00:00:00

  • Antitumor agents LV: Effects of genkwadaphnin and yuanhuacine on nucleic acid synthesis of P-388 lymphocytic leukemia cells.

    abstract::The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600711120

    authors: Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

    更新日期:1982-11-01 00:00:00

  • Forced degradation studies of corticosteroids with an alumina-steroid-ethanol model for predicting chemical stability and degradation products of pressurized metered-dose inhaler formulations.

    abstract::An alumina (Al(2)O(3))-steroid-ethanol model is used for forced degradation testing of corticosteroids to predict chemical stability and degradation products in pressurized metered-dose inhaler (pMDI) solution formulations. The model involves an ethanolic solution of a test steroid with Al(2)O(3), stressed at elevated...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23111

    authors: Wu ZZ,Thatcher ML,Lundberg JK,Ogawa MK,Jacoby CB,Battiste JL,Ledoux KA

    更新日期:2012-06-01 00:00:00

  • Physicochemical characterization of ricobendazole: I. Solubility, lipophilicity, and ionization characteristics.

    abstract::The physicochemical properties of ricobendazole (RBZ) were characterized using conventional methods. Solubility in some pharmaceutical solvents, pH-solubility, ionization properties, and lipophilicity are described. The solubility of RBZ in water is 62 mug/mL and very poor in common pharmaceutical solvents, for exampl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20282

    authors: Wu Z,Razzak M,Tucker IG,Medlicott NJ

    更新日期:2005-05-01 00:00:00

  • Impact of curcumin supersaturation in antibacterial photodynamic therapy--effect of cyclodextrin type and amount: studies on curcumin and curcuminoides XLV.

    abstract::Curcumin has been investigated as a potential photosensitizer (PS) in antimicrobial photodynamic therapy (aPDT). The phototoxic effect of curcumin is dependent on proper formulations of the compound because of the lipophilic nature of the molecule and the extremely low water solubility at physiological conditions. In ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23046

    authors: Hegge AB,Nielsen TT,Larsen KL,Bruzell E,Tønnesen HH

    更新日期:2012-04-01 00:00:00

  • Cerebral kinetics of oxycodone in conscious sheep.

    abstract::Oxycodone is an opioid analgesic that is administered orally or parenterally. The time-course of opioid action is a function of the systemic kinetics of the opioid, and the rate and extent of its entry into the brain and central nervous system. The latter is incompletely understood for oxycodone. Therefore, the cerebr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20632

    authors: Villesen HH,Foster DJ,Upton RN,Somogyi AA,Martinez A,Grant C

    更新日期:2006-08-01 00:00:00

  • Absence of povidone-iodine-induced mutagenicity in mice and hamsters.

    abstract::Povidone-iodine USP was tested for mutagenicity in mice by the dominant lethal assay or micronucleus test and in Chinese hamsters by the bone marrow test. None of the three tests revealed any evidence of mutagenic effect. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680133

    authors: Merkle J,Zeller H

    更新日期:1979-01-01 00:00:00

  • Combined use of pharmacokinetic modeling and a steady-state delivery approach allows early assessment of IkappaB kinase-2 (IKK-2) target safety and efficacy.

    abstract::NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21909

    authors: Chiang PC,Kishore NN,Thompson DC

    更新日期:2010-03-01 00:00:00

  • Dissolution profiles for finely divided drug suspensions.

    abstract::A suspension of micronized prednisolone acetate was separated into four fractions by the technique of centrifugal elutriation. Data showed that each fraction had a narrow particle size. The dissolution experiments were carried out under sink conditions (less than 10% of saturation concentration) in a dissolution appar...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720225

    authors: Mauger JW,Howard SA,Amin K

    更新日期:1983-02-01 00:00:00

  • Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000.

    abstract::Poor water solubility leads to low dissolution rate and consequently, it can limit bioavailability. Solid dispersions, where the drug is dispersed into an inert, hydrophilic polymer matrix can enhance drug dissolution. Solid dispersions were prepared using phenacetin and phenylbutazone as model drugs with polyethylene...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22613

    authors: Khan S,Batchelor H,Hanson P,Perrie Y,Mohammed AR

    更新日期:2011-10-01 00:00:00

  • Kinetics and mechanism of hydroxy group acetylations catalyzed by N-methylimidazole.

    abstract::The kinetics of acetylation of alcohols by acetyl chloride and acetic anhydride, with N-methylimidazole as the catalyst, were studied in acetonitrile solution at 25 degrees; some measurements were also made with 4-dimethylaminopyridine as the catalyst. The acetic anhydride-N-methylimidazole system proceeds entirely by...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710503

    authors: Pandit NK,Connors KA

    更新日期:1982-05-01 00:00:00

  • Electromigration of ions across the skin: determination and prediction of transport numbers.

    abstract::In iontophoresis, an electric field across the skin induces electromigration of exogenously applied and endogenously present ions. The approach can be used to improve dramatically drug delivery by elimination of competing co-ions in the externally applied formulation, as this maximizes the fraction of current carried ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20561

    authors: Mudry B,Guy RH,Delgado-Charro MB

    更新日期:2006-03-01 00:00:00

  • Interleukin-1 receptor antagonist: a new therapy for type 2 diabetes mellitus.

    abstract::Various complex mechanisms and their multifactorial pathways decisively provoke low-grade local and systemic inflammation in β-cells of pancreatic islets and peripheral tissues to induce β-cells' dysfunction and apoptosis, insulin resistance, and ultimately, overt type 2 diabetes mellitus (T2DM). Conventional antidiab...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.23057

    authors: Akash MS,Shen Q,Rehman K,Chen S

    更新日期:2012-05-01 00:00:00

  • Protein Nanoparticles Promote Microparticle Formation in Intravenous Immunoglobulin Solutions During Freeze-Thawing and Agitation Stresses.

    abstract::In this study, we investigated the potential roles of nanoparticles (<100 nm) and submicron (100-1000 nm) particles in the formation of microparticles (>1000 nm) in protein formulations under some pharmaceutically relevant stress conditions. Exposure of intravenous immunoglobulin solutions to the interface-associated ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.03.016

    authors: Pardeshi NN,Zhou C,Randolph TW,Carpenter JF

    更新日期:2018-07-01 00:00:00

  • High-pressure liquid chromatographic determination of cimetidine in plasma and urine.

    abstract::An assay is described for the determination of the H2-receptor antagonist, cimetidine, in human plasma and urine. Alkalinized plasma or urine was extracted with methylene chloride, the organic phase was evaporated, and the reconstituted residue was analysed by high-pressure liquid chromatography (HPLC) using a reverse...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710528

    authors: Mihaly GW,Cockbain S,Jones DB,Hanson RG,Smallwood RA

    更新日期:1982-05-01 00:00:00

  • Scintigraphic evaluation of a new capsule-type colon specific drug delivery system in healthy volunteers.

    abstract::Colonic drug delivery is intended for local or systemic therapies. The lack of predictive in vitro or animal model leads to considerable time delays in colonic product development. The objective of this scintigraphic study was to provide "proof of concept" for a novel capsule-type colonic delivery system (Colon-Target...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1021/js9704588

    authors: Ishibashi T,Pitcairn GR,Yoshino H,Mizobe M,Wilding IR

    更新日期:1998-05-01 00:00:00

  • Enrichment of Relevant Oxidative Degradation Products in Pharmaceuticals With Targeted Chemoselective Oxidation.

    abstract::The ability to produce and isolate relatively pure amounts of relevant degradation products is key to several aspects of drug product development: (a) aid in the unambiguous structural identification of such degradation products, fulfilling regulatory requirements to develop safe formulations (International Conference...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.10.059

    authors: Nanda KK,Mozziconacci O,Small J,Allain LR,Helmy R,Wuelfing WP

    更新日期:2019-04-01 00:00:00

  • Exploring a Kinetic Model Approach in Biopharmaceutics: Estimating the Fraction Absorbed of Orally Administered Drugs in Humans.

    abstract::Increasing costs of research and development in the pharmaceutical industry has necessitated a growing interest in the early prediction of human pharmacokinetics of drug candidates. Of growing interest is the need to understand oral absorption, the most common route of small molecule drug administration. The fraction ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.03.015

    authors: Chiang PC,Liu J,Fan P,Wong H

    更新日期:2018-07-01 00:00:00

  • Factors Influencing the Retention of Organic Solvents in Products Freeze-Dried From Co-Solvent Systems.

    abstract::Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2018.04.001

    authors: Kunz C,Gieseler H

    更新日期:2018-08-01 00:00:00

  • Improved delivery through biological membranes XIX: Novel redox carriers for brain-specific chemical delivery systems.

    abstract::New dihydropyridine in equilibrium pyridinium salt-type redox carrier systems were developed in which the drug is linked via the ring nitrogen atom of nicotinamide. The rate of oxidation of the dihydropyridine forms, and thus the overall and brain-specific distribution of the corresponding 3-carbamoyl-1-carbamoylalkyl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740304

    authors: Bodor N,AbdelAlim AM

    更新日期:1985-03-01 00:00:00

  • Synthesis and binding to beta-adrenergic receptors of p-aminobenzyl analogues of practolol and atenolol.

    abstract::The p-aminobenzyl analogues (8a and 8b, respectively) of the cardioselective beta-adrenergic receptor antagonists practolol and atenolol were prepared from the corresponding phenoxymethyloxiranes in 30 and 13% yields, respectively. The dissociation constants for the beta-adrenergic receptor were measured in membrane p...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810422

    authors: Jones GS Jr,Bylund DB,Hanson RN

    更新日期:1992-04-01 00:00:00

  • Calorimetric relaxation and the glass-liquid temperature range of acetaminophen-nifedipine alloys.

    abstract::Glassy states of nine acetaminophen-nifedipine compositions have been made by slowly supercooling their melts, and calorimetric T(g) and the nonexponential, nonlinear relaxation parameters beta and x that are used in modeling the mobility of a pharmaceutical determined. The T(g)-endotherm's shape varies with the alloy...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21252

    authors: Johari GP,Shanker RM

    更新日期:2008-08-01 00:00:00

  • Comparison of operational characteristics of different dissolution testing systems.

    abstract::Three dissolution apparatus, the rotating basket, the rotating paddle, and the rotating filter--stationary basket, were evaluated for their suitability as production control tools and their relation to blood level studies in dogs. The rotating basket and rotating paddle assemblies were easier to use and less variable ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600671226

    authors: Hardwidge EA,Sarapu AC,Laughlin WC

    更新日期:1978-12-01 00:00:00

  • Formulation and evaluation of quercetin polycaprolactone microspheres for the treatment of rheumatoid arthritis.

    abstract::Quercetin had been shown to be effective in the management of arthritis. However, bioavailability of quercetin is a concern for such treatment. This work aims at the development of intra-articular drug delivery system by controlled release of quercetin (loaded in microspheres) for the management of rheumatoid arthriti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22266

    authors: Natarajan V,Krithica N,Madhan B,Sehgal PK

    更新日期:2011-01-01 00:00:00

  • Use of fluorometry in assessing the efficacy of a cation-sensitive gel as an ophthalmic vehicle: comparison with scintigraphy.

    abstract::Gelrite, a heteropolysaccharide that forms a gel in the presence of cations, was tested in humans for its efficacy as an ophthalmic vehicle by a nonivasive fluorometric technique. Fluorescein was used as the tracer, and its concentration in the anterior chamber was used as the principal measure of bioavailability. The...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810704

    authors: Maurice DM,Srinivas SP

    更新日期:1992-07-01 00:00:00

  • The future of protein particle characterization and understanding its potential to diminish the immunogenicity of biopharmaceuticals: a shared perspective.

    abstract::Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23247

    authors: Bee JS,Goletz TJ,Ragheb JA

    更新日期:2012-10-01 00:00:00

  • Determination of diphenoxylate hydrochloride and atropine sulfate in solutions and tablets.

    abstract::Methods for the determination of diphenoxylate hydrochloride and atropine sulfate combinations in solutions and powdered tablet composites are presented. A semiautomated assay for diphenoxylate hydrochloride in individual tablets (content uniformity) also is presented. The USP XIX assays for these products are cumbers...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600661113

    authors: Ballbach RL,Brown DJ,Walters SM

    更新日期:1977-11-01 00:00:00