Effect of low molecular weight chitosans on drug permeation through mouse skin: 1. Transdermal delivery of baicalin.

Abstract:

:The aim of this work was to evaluate the low molecular weight chitosans (LMWCs) as enhancers of transdermal administration of baicalin, an useful drug for the treatment of atopic dermatitis, viral hepatitis, and HIV infection. Permeation experiments were performed in vitro through mouse skin by using Franz cells. Improved baicalin skin penetration was obtained with the addition of LMWCs or D-glucosamine (beta-D-GlcNH(2)) to the donor solutions. Chitosan molecular weight, degree of deacetylation, pH of donor baicalin solutions, and enhancer concentration all affected LMWC enhancement effects. Significant enhancement was observed at pH 7.0 or 7.5 for CS80-1000, and the enhancement factor (EF) in the co-delivery method was calculated as 11.7 or 15.9, respectively. Simultaneously, beta-D-GlcNH(2) showed greatest enhancement at pH 7.0 with an EF of 11. Moreover, there was an optimal concentration range (0.5-1% by weight for CS80-1000 and 1.0-1.5% for beta-D-GlcNH(2)) to enhance baicalin transdermal delivery. It was concluded that the effective fractions for the enhancement of LMWCs were beta-D-GlcNH(2) oligomers, and the repeated number of beta-D-GlcNH(2) was suggested to be in the range 2-6. Enhancement mechanism of LMWCs was also discussed and suggested to be relative to the interactions of LMWC with both baicalin and the lipid of stratum corneum.

journal_name

J Pharm Sci

authors

Zhou X,Liu D,Liu H,Yang Q,Yao K,Wang X,Wang L,Yang X

doi

10.1002/jps.22063

subject

Has Abstract

pub_date

2010-07-01 00:00:00

pages

2991-8

issue

7

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)32559-4

journal_volume

99

pub_type

杂志文章
  • Frog intestinal sac: a new in vitro method for the assessment of intestinal permeability.

    abstract::The aim of this study was to evaluate a new experimental protocol utilizing isolated frog intestinal sacs for the assessment of intestinal drug permeability in humans. Segments of approximately 5.0 cm in length were used for these experiments. The intestinal sacs were filled with a solution of the appropriate drug in ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20180

    authors: Trapani G,Franco M,Trapani A,Lopedota A,Latrofa A,Gallucci E,Micelli S,Liso G

    更新日期:2004-12-01 00:00:00

  • Distribution and elimination of polymethyl methacrylate nanoparticles after peroral administration to rats.

    abstract::Polymethyl [1-14C]methacrylate nanoparticles were administered orally to bile cannulated rats. Ten to fifteen percent of the administered radioactivity was absorbed and found in the bile and urine. Within 48 h, 94-97% of the absorbed radioactivity had been eliminated from the body. After 8 d, the highest residual radi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730934

    authors: Nefzger M,Kreuter J,Voges R,Liehl E,Czok R

    更新日期:1984-09-01 00:00:00

  • Perfluorooctyl bromide concentration in plasma and tissues of beagle dogs.

    abstract::Plasma levels were determined frequently after single doses of perfluorooctyl bromide were administered to beagle dogs at doses of either 30.8 g/kg po or 3.9 g/kg intratracheally. The apparent first-order half-life during the terminal elimination phase was about 1 day after oral medication and about 7 days after intra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670751

    authors: Lee FH,Scrime M,Edelson J

    更新日期:1978-07-01 00:00:00

  • My mentors.

    abstract::This paper traces the academic genealogy of Professor Takeru Higuchi, who is considered "The Father of Physical Pharmacy" because of his contributions to the science of drug formulation and delivery and his impact in mentoring a whole generation of post-World War II pharmaceutical scientists. As one who was mentored b...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 传,社论,历史文章

    doi:10.1002/jps.1049

    authors: Stella VJ

    更新日期:2001-08-01 00:00:00

  • Determination of the chemical constituents and spectral properties of commercial and NF reference standard potassium guaiacolsulfonate: implications of the findings on compendial analytical methodology.

    abstract::HPLC analysis confirmed a difference in the chemical composition of commercial versus NF reference standard potassium guaiacolsulfonate. After separation by fractional crystallization, the two constituents comprising the former sample were identified by 1H-NMR as potassium guaiacol-4- and -5-sulfonate, respectively. T...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730911

    authors: Tangtatsawasdi P,Krikorian SE

    更新日期:1984-09-01 00:00:00

  • Osmotic water transport through cellulose acetate membranes produced from a latex system.

    abstract::The advisability of a progressive curtailment of organic solvent film coating offers an incentive to develop latex systems. Here, the use of aqueous colloidal dispersions of cellulose acetate, plasticized with water-soluble additives, is proposed as an alternative way to obtain cellulose acetate membranes either by ca...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600760609

    authors: Bindschaedler C,Gurny R,Doelker E

    更新日期:1987-06-01 00:00:00

  • TLC differentiation of butyrophenone and diphenylbutylpiperidine compounds from phenothiazine derivatives.

    abstract::A procedure is described for TLC detection and differentiation of the butyrophenone-diphenylbutylpiperidine group and phenothiazine derivatives at the microgram level. A two-dimensional TLC method to separate butyrophenone and diphenylbutylpiperidine compounds is reported. A variety of possible detection reagents were...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680834

    authors: Pluym A

    更新日期:1979-08-01 00:00:00

  • Evaluation of Systemic and Mucosal Immune Responses Induced by a Nasal Powder Delivery System in Conjunction with an OVA Antigen in Cynomolgus Monkeys.

    abstract::An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.11.023

    authors: Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

    更新日期:2020-12-03 00:00:00

  • Effect of buffer species on the thermally induced aggregation of interferon-tau.

    abstract::It is now becoming apparent that a common pathway of protein aggregation involves the unimolecular structural rearrangement from the native state to a slightly expanded aggregation-competent species. It is the goal of this study to understand the aggregation and the effects of buffer on the stability of IFN-tau. In th...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20471

    authors: Katayama DS,Nayar R,Chou DK,Valente JJ,Cooper J,Henry CS,Vander Velde DG,Villarete L,Liu CP,Manning MC

    更新日期:2006-06-01 00:00:00

  • Modified cellulose II powder: preparation, characterization, and tableting properties.

    abstract::The reaction of UICEL-A/102, a cellulose II powder recently prepared from Avicel(R) PH-102 by treatment with an aqueous sodium hydroxide solution, with glutaraldehyde in 0.01 N HCl has been investigated to improve its binder properties, without adversely affecting the rapid disintegration characteristic. The results s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20747

    authors: de la Luz Reus Medina M,Kumar V

    更新日期:2007-02-01 00:00:00

  • Synthesis and evaluation of Ketorolac ester prodrugs for transdermal delivery.

    abstract::Alkyl esters of ketorolac were synthesized as potential prodrugs for transdermal delivery and evaluated to determine the relationship between their skin permeation characteristics and their physicochemical properties. Solubility of the prodrugs in various vehicles was determined at room temperature while lipophilicity...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10353

    authors: Doh HJ,Cho WJ,Yong CS,Choi HG,Kim JS,Lee CH,Kim DD

    更新日期:2003-05-01 00:00:00

  • Comparison of In Vivo Transportability of Anti-Methicillin-Resistant Staphylococcus aureus (MRSA) Agents Into Intracellular and Extracellular Tissue Spaces in Rats.

    abstract::The pathogenic bacterium Staphylococcus aureus can penetrate host cells. However, intracellular S. aureus is not considered during antimicrobial agent selection in clinical chemotherapy because of the lack of information about drug transportability into cells in vivo. We focused on agents used to treat methicillin-res...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.09.045

    authors: Kobuchi S,Kita Y,Hiramatsu Y,Sasaki K,Uno T,Ito Y,Sakaeda T

    更新日期:2021-02-01 00:00:00

  • Interactions of cyclosporines with lipid membranes as studied by solid-state nuclear magnetic resonance spectroscopy and high-sensitivity titration calorimetry.

    abstract::Cyclosporin A (CyA) interacts with lipid membranes. Binding reaction and membrane location of CyA and analogs were examined with 2H-NMR, high-sensitivity isothermal titration calorimetry (ITC), and CD spectroscopy. Effects of CyA and charged analogs on the phosphocholine head group and on the membrane interior were in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10071

    authors: Schote U,Ganz P,Fahr A,Seelig J

    更新日期:2002-03-01 00:00:00

  • Limits on optimizing ocular drug delivery.

    abstract::The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600800113

    authors: Keister JC,Cooper ER,Missel PJ,Lang JC,Hager DF

    更新日期:1991-01-01 00:00:00

  • In Vivo Fluid Volume in Rat Gastrointestinal Tract: Kinetic Analysis on the Luminal Concentration of Nonabsorbable FITC-Dextran After Oral Administration.

    abstract::Previously, 1 mL of purified water (hyposmotic) or saline (isosmotic) which dissolved 200 μM of FITC-dextran (FD-4), a nonabsorbable marker, was orally administered to rats, and luminal concentration-time profile of FD-4 was directly measured. In this study, at first, luminal FD-4 concentration was measured after oral...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.03.005

    authors: Tanaka Y,Higashino H,Kataoka M,Yamashita S

    更新日期:2020-06-01 00:00:00

  • An efficient approach for the rapid assessment of oral rat exposures for new chemical entities in drug discovery.

    abstract::Present study aims to improve efficiency and capacity of in vivo rat pharmacokinetic studies for rapid assessment of systemic exposure (AUC and C(max)) of new chemical entities. Plasma concentration-time profiles in rats from structurally diverse compounds were extracted from the Pfizer database. AUC(0-8) was calculat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20642

    authors: Han HK,Sadagopan N,Reichard GA,Yapa U,Zhu T,Hubbel A,Johnson K,Brodfuehrer J

    更新日期:2006-08-01 00:00:00

  • Pharmacokinetic study of (S)-(-)-2-(N-propyl-N-(2-thienylethyl)amino)-5-hydroxytetralin infusion in cynomolgus monkeys.

    abstract::A pharmacokinetic study of the dopamine D2 receptor agonist (S)-(-)-2-(N-propyl-N-(2-thienylethyl)amino)-5-hydroxytetralin+ ++-HCl (N-0923) infused in female cynomolgus monkeys over a 4-h period was carried out at International Research and Development Corporation. The purpose of this study was to estimate the elimina...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600830533

    authors: Walters DR,McConnell WR,Cefali EA

    更新日期:1994-05-01 00:00:00

  • Anticonvulsant activity of some 4-methoxy- and 4-chlorobenzanilides.

    abstract::A series of mono-, di-, and trimethylated derivatives of 4-chloro- and 4-methoxybenzanilide was synthesized and evaluated for anticonvulsant activity. This series was prepared in the course of studies designed to examine the relationship between anticonvulsant effects and benzamide structure. The compounds were tested...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790308

    authors: Clark CR,McMillian CL

    更新日期:1990-03-01 00:00:00

  • In situ monitoring of polymorph transformation of clopidogrel hydrogen sulfate using measurement of ultrasonic velocity.

    abstract::Transformation of polymorph I of clopidogrel hydrogen sulfate (CHS) to polymorph II of CHS during the crystallization was monitored by using in situ measurement of ultrasonic velocity. Drowning-out crystallization using methanol as a solvent and isopropyl alcohol as nonsolvent was carried out. The polymorphs were iden...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21313

    authors: Kim HJ,Kim KJ

    更新日期:2008-10-01 00:00:00

  • Neglected populations: safeguarding the health of street-involved children in Ghana.

    abstract::Ensuring the health of street-involved children is a growing public health challenge. These children are vulnerable, neglected, and rarely a priority for basic service providers and governments. Sizable populations of street-involved children are present in major urban areas worldwide and current trends in urbanizatio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23255

    authors: Osei-Twum JA,Wasan KM

    更新日期:2012-10-01 00:00:00

  • Pharmacokinetic aspects of biotechnology products.

    abstract::In recent years, biotechnologically derived peptide and protein-based drugs have developed into mainstream therapeutic agents. Peptide and protein drugs now constitute a substantial portion of the compounds under preclinical and clinical development in the global pharmaceutical industry. Pharmacokinetic and exposure/r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.20125

    authors: Tang L,Persky AM,Hochhaus G,Meibohm B

    更新日期:2004-09-01 00:00:00

  • Pharmacokinetics of dopamine-2 agonists in rats and dogs.

    abstract::The absorption, protein binding, blood-to-plasma ratio, renal excretion, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone (1), N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide (2), and 4-(2-di-n-propylaminoethyl)-2-(3H)-indolone (3...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600751002

    authors: Swagzdis JE,Wittendorf RW,DeMarinis RM,Mico BA

    更新日期:1986-10-01 00:00:00

  • Unexpected performance of physical mixtures over solid dispersions on the dissolution behavior of benznidazole from tablets.

    abstract::This work investigated the feasibility of developing benznidazole (BZL) tablets, allowing fast, reproducible, and complete drug dissolution, by compressing BZL-Polyethylene Glycol (PEG) 6000 physical mixtures (PMs) and solid dispersions (SDs). SDs were prepared by the solvent evaporation method at different drug:polym...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23448

    authors: Leonardi D,Salomon CJ

    更新日期:2013-03-01 00:00:00

  • Determination of dextromethorphan hydrobromide by high-performance liquid chromatography using ion-pair formation.

    abstract::The chromatographic retention behavior of dextromethorphan hydrobromide on an octadecylsilane column was investigated as a function of the pairing ion and the mobile phase composition. Dramatic increases in the capacity factor were observed with pairing ions containing more than eight carbons and with decreasing organ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600691207

    authors: Kubiak EJ,Munson JW

    更新日期:1980-12-01 00:00:00

  • Synthesis of alkylaminoalkylamides of substituted 2-aminopyrroles as potential local anesthetic and antiarrhythmic agents. II: beta-Amines.

    abstract::The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 14 2-(3-alkylaminoalkylamido)-pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, with seven showing comparable or greater activity than lidocaine. Most compounds also exhibite...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700519

    authors: Sowell JW Sr,Block AJ,Derrick ME,Freeman JJ,Kosh JW,Mubarak PF,Tenthorey PA

    更新日期:1981-05-01 00:00:00

  • Acetaminophen inhibits intestinal p-glycoprotein transport activity.

    abstract::Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23673

    authors: Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

    更新日期:2013-10-01 00:00:00

  • Apparent absorption kinetics of micronized griseofulvin after its oral administration on single- and multiple-dose regimens to rats as a corn oil-in-water emulsion and aqueous suspension.

    abstract::This investigation was designed to quantitate and compare in the rat the oral absorption characteristics of micronized griseofulvin from a corn oil-in-water emulsion dosage form containing suspended drug and a control aqueous suspension after single-dose (50 mg/kg) and multiple-dose (50 mg/kg every 12 hr for five dose...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600640910

    authors: Bates TR,Carrigan PJ

    更新日期:1975-09-01 00:00:00

  • Effect of milling and compression on the solid-state Maillard reaction.

    abstract::The effects of milling and compression on the solid-state Maillard reaction between metoclopramide hydrochloride and lactose were investigated. Anhydrous metoclopramide hydrochloride was milled for various times, and then mixed with amorphous lactose. The mixtures were stored at 105 degrees C and 0% RH. The reactivity...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20448

    authors: Qiu Z,Stowell JG,Cao W,Morris KR,Byrn SR,Carvajal MT

    更新日期:2005-11-01 00:00:00

  • Soft gelatin capsules II: Oxygen permeability study of capsule shells.

    abstract::A method is reported for studying the effects of several factors at room temperature on the oxygen permeability of soft gelatin capsule shell films. The method involves the use of a permeability cell assembly and the spectrophotometric determïnation of oxygen with an alkaline pyrogallic acid solution. Factors investig...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600640528

    authors: Hom FS,Veresh SA,Ebert WR

    更新日期:1975-05-01 00:00:00

  • Colloidal and thermal characteristics of concentrated dispersions of polymethacrylate-based latices for aqueous enteric coating.

    abstract::We have used rheological and thermal methods to study the colloidal characteristics of a widely used technical latex. The dispersions of poly(methacrylic acid-ethyl acrylate) (Eudragit L100-55) were found to be stabilized by a combination of electrostatic and steric mechanisms termed as electrosteric stabilization. Th...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9803555

    authors: Paulsson M,Singh SK

    更新日期:1999-04-01 00:00:00