Polyamidoamine dendrimers can improve the pulmonary absorption of insulin and calcitonin in rats.

Abstract:

:The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absorption with or without PAMAM dendrimers was examined by in vivo pulmonary absorption studies. PAMAM dendrimers significantly increased the pulmonary absorption of insulin and calcitonin in rats, and their absorption-enhancing effects were generation dependent. The rank order of absorption enhancement effect of these PAMAM dendrimers was G3 > G2 > G1 > G0. For the same generation, the absorption-enhancing effects of PAMAM dendrimers were shown to be concentration dependent. The toxicity of these PAMAM dendrimers in the lung tissues was evaluated by measuring the release of protein and the activities of lactate dehydrogenase (LDH) in bronchoalveolar lavage fluid (BALF). The PAMAM dendrimers with various generations and concentrations did not significantly increase the release of protein and the activities of LDH in BALF, indicating that these dendrimers did not cause any membrane damage to the lung tissues. The zeta potentials of insulin and calcitonin solutions changed to positive by the addition of PAMAM dendrimers, and the degree of positive charge as determined by the zeta potentials was linearly correlated with the absorption-enhancing effects of the PAMAM dendrimers. This positive charge of the PAMAM dendrimers might be related to their absorption-enhancing mechanisms for improving the pulmonary absorption of insulin and calcitonin in rats. In conclusion, the PAMAM dendrimers are suitable absorption enhancers to improve the pulmonary absorption of insulin and calcitonin without any membrane damage to the respiratory tissues.

journal_name

J Pharm Sci

authors

Dong Z,Hamid KA,Gao Y,Lin Y,Katsumi H,Sakane T,Yamamoto A

doi

10.1002/jps.22428

subject

Has Abstract

pub_date

2011-05-01 00:00:00

pages

1866-78

issue

5

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)32178-X

journal_volume

100

pub_type

杂志文章
  • Solubility, ionization, and partitioning behavior of unsymmetrical disulfide compounds: alkyl 2-imidazolyl disulfides.

    abstract::Alkyl 2-imidazolyl disulfide compounds are novel antitumor agents, one of which is currently being evaluated in Phase I clinical trials. These molecules contain an unsymmetrical disulfide fragment, the lipophilic and electronic contributions of which are still not defined in the literature. Lipophilicity, ionization, ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10112

    authors: Hashash A,Kirkpatrick DL,Lazo JS,Block LH

    更新日期:2002-07-01 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

    doi:10.1002/jps.10173

    authors: Segarra I,Movshin DA,Zarif L

    更新日期:2002-08-01 00:00:00

  • Preparation and characterization of a customized cellulose acetate butyrate dispersion for controlled drug delivery.

    abstract::The purpose of the present experiment was to prepare and characterize the aqueous-based pseudolatex system of cellulose acetate butyrate (CAB) for controlled drug delivery. Aqueous pseudolatex systems are advantageous over organic-based coating systems because these systems are devoid of criteria pollutants such as ca...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10155

    authors: Vaithiyalingam S,Nutan M,Reddy I,Khan M

    更新日期:2002-06-01 00:00:00

  • Thai Silk Fibroin/Gelatin Sponges for the Dual Controlled Release of Curcumin and Docosahexaenoic Acid for Anticancer Treatment.

    abstract::In this study, curcumin and/or docosahexaenoic acid (DHA) were encapsulated in Thai silk fibroin/gelatin (SF/G) sponges, prepared at different blending ratios, aimed to be applied as a controlled release system for localized cancer therapy. The SF/G sponges were fabricated by freeze-drying and glutaraldehyde cross-lin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24701

    authors: Lerdchai K,Kitsongsermthon J,Ratanavaraporn J,Kanokpanont S,Damrongsakkul S

    更新日期:2016-01-01 00:00:00

  • GLC determination of cyclobenzaprine in plasma and urine.

    abstract::A GLC determination of cyclobenzaprine in human plasma and urine is described. After extraction from alkalinized samples with heptane-isopentyl alcohol (97:3), the drug and internal standard were back-extracted into 0.1 N HCl and then reextracted into ether. Use of a lower homolog of the drug as an internal standard w...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650832

    authors: Hucker HB,Stauffer SC

    更新日期:1976-08-01 00:00:00

  • Bioavailability of 17 ampicillin products.

    abstract::The bioavailability of single lots of 250-mg ampicillin capsules, available from 17 distributors and/or manufactures, was determined. Each product was evaluated in terms of the serum ampicillin levels achieved at 1, 2, 3, 4, 6, and 8 hr postadministration, the peak serum levels, the time of peak serum level, and the a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650505

    authors: Whyatt PL,Slywka GW,Melikian AP,Meyer MC

    更新日期:1976-05-01 00:00:00

  • Effect of individual Fc methionine oxidation on FcRn binding: Met252 oxidation impairs FcRn binding more profoundly than Met428 oxidation.

    abstract::The long serum half-lives of mAbs are conferred by pH-dependent binding of IgG-Fc to the neonatal Fc receptor (FcRn). The Fc region of human IgG1 has three conserved methionine residues, Met252, Met358, and Met428. Recent studies showed oxidation of these Met residues impairs FcRn binding and consequently affects phar...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24136

    authors: Gao X,Ji JA,Veeravalli K,Wang YJ,Zhang T,Mcgreevy W,Zheng K,Kelley RF,Laird MW,Liu J,Cromwell M

    更新日期:2015-02-01 00:00:00

  • Preparation and Characterization of Ascosome Vesicles Loaded with Khellin.

    abstract::Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.06.017

    authors: Risaliti L,Ambrosi M,Calamante M,Bergonzi MC,Lo Nostro P,Bilia AR

    更新日期:2020-10-01 00:00:00

  • Epimeric 5-hydroxy-5-phenyl-1-azabicyclo [5.4.0] undecanes.

    abstract::The development of order during the aging of aluminum hydroxide gel prepared by the reaction of aluminum chloride and ammonium hydroxide to a final pH of 7.0 can be monitored by differential thermal analysis. The loss fo acid reactivity upon aging is accompanied by an increase in the temperature and intensity of the d...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650931

    authors: Aboul-Enein N,Sam J

    更新日期:1976-09-01 00:00:00

  • Paired-ion reversed-phase high-pressure liquid chromatographic assay of pentobarbital-pyrilamine suppositories.

    abstract::The assay of suppositories containing pentobarbital and/or pyrilamine in a water-soluble polyethylene glycol base by high-pressure liquid chromatography is described. No extraction is required. The suppository is dissolved in the mobile phase. This solution is diluted with an internal standard stock solution containin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680524

    authors: Block JH,Levine HL,Ayres JW

    更新日期:1979-05-01 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

    doi:10.1002/jps.23975

    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

  • Determination of total pyridoxal in human plasma following oral administration of vitamin B6 by high-performance liquid chromatography with post-column derivatization.

    abstract::An HPLC method for determining total pyridoxal from plasma was developed for a relative bioavailability comparison of two oral vitamin B6 (pyridoxine HCl) preparations. After cleavage of the pyridoxal-5-phosphate with the acid phosphatase enzyme, the total pyridoxal was determined by HPLC. Pyridoxal was separated on a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820921

    authors: Mascher H

    更新日期:1993-09-01 00:00:00

  • GLC determination of procainamide in biological fluids.

    abstract::A GLC method for the determination of procainamide in biological fluids is presented. By using a dipropyl analog of procainamide as an internal standard, both compounds can be chromatographed directly, yielding linear calibration curves and a sensitivity that allows quantitative determination of concentrations as low ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600641213

    authors: Simons KJ,Levy RH

    更新日期:1975-12-01 00:00:00

  • Impact of Precipitation of Antibody Therapeutics After Subcutaneous Injection on Pharmacokinetics and Immunogenicity.

    abstract::Antibody therapeutics with poor solubility in the subcutaneous matrix may carry unintended risks when administered to patients. The objective of this work was to estimate the risk of antibodies that precipitate in vitro at neutral pH by determining the impact of poor solubility on distribution of the drug from the inj...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.01.015

    authors: Kinderman F,Yerby B,Jawa V,Joubert MK,Joh NH,Malella J,Herskovitz J,Xie J,Ferbas J,McBride HJ

    更新日期:2019-06-01 00:00:00

  • Extended least squares (ELS) for pharmacokinetic models.

    abstract::An important part of pharmacokinetic research is fitting models to observed data and estimating the parameters in the model. In general, parameter estimation in pharmacokinetics is a subset of the general problem of nonlinear regression or parameter estimation in nonlinear regression models. The same criteria, algorit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600760716

    authors: Metzler CM

    更新日期:1987-07-01 00:00:00

  • PATH's approach to product introduction in developing countries.

    abstract::Health interventions developed for wealthy nations are difficult to introduce in developing countries due to a lack of sufficient technological, financial, political, or infrastructural resources. Increasingly, however, product developers are creating new technologies that meet the needs of low-resource settings. Expe...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21364

    authors: Harner-Jay C,Sherris J

    更新日期:2008-12-01 00:00:00

  • Pharmacokinetic study of methotrexate following intra-articular injection of methotrexate loaded poly(L-lactic acid) microspheres in rabbits.

    abstract::The pharmacokinetics and tissue distribution of methotrexate (MTX) were investigated following intra-articular injection of either MTX solution or controlled release MTX loaded microspheres in healthy rabbit joints. MTX solution or MTX loaded microspheres (size 30-100 mum) (10 mg MTX) was injected into the right knee ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20341

    authors: Liang LS,Wong W,Burt HM

    更新日期:2005-06-01 00:00:00

  • Preparation of in situ-forming ophthalmic gels of ciprofloxacin hydrochloride for the treatment of bacterial conjunctivitis: in vitro and in vivo studies.

    abstract::Sol-to-gel systems of ciprofloxacin hydrochloride were prepared utilizing the phase transition properties of hydroxy propyl methyl cellulose K 15 M grade (HPMC) and carbopol 934. The sol-to-gel systems were sterilized by gamma radiation and/or filtration. The sol-to-gel systems were evaluated for rheological character...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10290

    authors: Charoo NA,Kohli K,Ali A

    更新日期:2003-02-01 00:00:00

  • Quantitative determinations of two decongestants and an antihistamine in combination using paired ion high-pressure liquid chromatography.

    abstract::A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670643

    authors: Ghanekar AG,Das Gupta V

    更新日期:1978-06-01 00:00:00

  • Quantitative Estimation of Plasma Free Drug Fraction in Patients With Varying Degrees of Hepatic Impairment: A Methodological Evaluation.

    abstract::Quantitative prediction of unbound drug fraction (fu) is essential for scaling pharmacokinetics through physiologically based approaches. However, few attempts have been made to evaluate the projection of fu values under pathological conditions. The primary objective of this study was to predict fu values (n = 105) of...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.02.021

    authors: Li GF,Yu G,Li Y,Zheng Y,Zheng QS,Derendorf H

    更新日期:2018-07-01 00:00:00

  • Evaluation of PEGylated exendin-4 released from poly (lactic-co-glycolic acid) microspheres for antidiabetic therapy.

    abstract::Peptide-based therapies have the potential to induce antibody formation if the molecules differ from a native human peptide. Several reports have disclosed the occurrence of antibody generation in a patient treated with exenatide. The immune response can be problematic from a clinical stand point, particularly if the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24238

    authors: Lim SM,Eom HN,Jiang HH,Sohn M,Lee KC

    更新日期:2015-01-01 00:00:00

  • Chemical modifications of therapeutic proteins induced by residual ethylene oxide.

    abstract::Ethylene oxide (EtO) is widely used in sterilization of drug product primary containers and medical devices. The impact of residual EtO on protein therapeutics is of significant interest in the biopharmaceutical industry. The potential for EtO to modify individual amino acids in proteins has been previously reported. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24257

    authors: Chen L,Sloey C,Zhang Z,Bondarenko PV,Kim H,Ren D,Kanapuram S

    更新日期:2015-02-01 00:00:00

  • A solid-state NMR study of phase structure, molecular interactions, and mobility in blends of citric acid and paracetamol.

    abstract::Citric acid anhydrate (CAA) and paracetamol (PARA), prepared as crystalline physical mixtures and as amorphous blends, were studied using (13)C solid-state cross polarization magic angle spinning (CPMAS) NMR. Amorphous blends showed significant line broadening from the conformational distribution as compared to the cr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21559

    authors: Schantz S,Hoppu P,Juppo AM

    更新日期:2009-05-01 00:00:00

  • In vitro release and intestinal absorption of physostigmine salicylate from submicron emulsions.

    abstract::The in vitro release of physostigmine salicylate (PS) from a submicron emulsion and an aqueous solution was studied using the dialysis bag method. These formulations were then perfused to various locations along the rat small intestine (proximal, mid, and distal jejunum), and two lengths (10 and 55 cm). The disappeara...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600800706

    authors: Rubinstein A,Pathak YV,Kleinstern J,Reches A,Benita S

    更新日期:1991-07-01 00:00:00

  • Synthesis of d-pilocarpine-N-14CH3.

    abstract::The total synthesis of d-pilocarpine specifically labeled as N-14CH3 is reported. dl-Homopilopic acid was prepared as a key intermediate and resolved into the d-enantiomer via the alpha-methylbenzylamine salt. The penultimate intermediate, 2-mercaptopilocarpine, was desulfurized by oxidation with dilute hydrogen perox...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600641026

    authors: DeGraw JI,Engstrom JS,Willis E

    更新日期:1975-10-01 00:00:00

  • Peptide derivation of poorly absorbable drug allows intestinal absorption via peptide transporter.

    abstract::The purpose of the present study was to examine whether the intestinal absorption of low-permeability drugs could be improved by utilization of the intestinal influx transporter PEPT1. We investigated whether peptide derivatives of poorly absorbable nonamino acid-like drugs might be substrates of PEPT1, using rebamipi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21551

    authors: Kikuchi A,Tomoyasu T,Tanaka M,Kanamitsu K,Sasabe H,Maeda T,Odomi M,Tamai I

    更新日期:2009-05-01 00:00:00

  • Design of Hollow Hyaluronic Acid Cylinders for Sustained Intravitreal Protein Delivery.

    abstract::A hollow cylinder intravitreal implant was developed to achieve sustained release of protein to the retina for the treatment of retinal diseases. Hollow cylinders were fabricated by molding and cross-linking hyaluronic acid, the major component of the vitreous humor. Hollow cylinders were filled with a concentrated pr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.04.024

    authors: Van Kampen E,Vandervelden C,Fakhari A,Qian J,Berkland C,Gehrke SH

    更新日期:2018-09-01 00:00:00

  • Effect of symmetrical tetraalkylammonium salts on cloud point on nonionic surfactants.

    abstract::The salting in and salting out of the nonionic surfactant octoxynol NF by halides of ammonium and the four lowest symmetrical tetraalkylammonium cations were investigated by measuring their effect on the cloud point at various salt concentrations. The chloride anion tended to salt the surfactant out, lowering its clou...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660208

    authors: Schott H,Han SK

    更新日期:1977-02-01 00:00:00

  • Synthesis of 4,5-dimethoxykynuramine and its in vivo conversion to 6,7-dimethoxy-4-quinolinol.

    abstract::4,5-Dimethoxykynuramine was synthesized in a three-step sequence originating with veratrole. Indirect evidence indicates that the drug was converted in vivo to the hypotensive agent 6,7-dimethoxy-4-quinolinol by the action of monoamine oxidase. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670344

    authors: Schwan TJ,Honkomp LJ,Snyder HR Jr,Watson EJ

    更新日期:1978-03-01 00:00:00

  • Synthesis, cytotoxicity, hypolipidemic and anti-inflammatory activities of amine-boranes and esters of boron analogues of choline and thiocholine.

    abstract::Boron analogues of carbamoylcholine and thiocholine and esters of these analogues were prepared. These compounds were fairly stable toward hydrolysis and demonstrated moderate anti-inflammatory and hypolipidemic activities in mice. The hypolipidemic activity of the compounds at a dose of 8 mg/kg/day was equivalent in ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810514

    authors: Sood A,Sood CK,Spielvogel BF,Hall IH,Wong OT

    更新日期:1992-05-01 00:00:00