Abstract：
PURPOSE:The investigation was aimed at developing micellar nanocarriers for nose-to-brain delivery of zolmitriptan with the objective to investigate the pathway involved in the drug transport. METHODS:The micellar nanocarrier was successfully formulated and characterized for particle size and shape by multi-angle dynamic light scattering, small angle neutron scattering and cryo-transmission electron microscopy. Toxicity and biodistribution studies were carried out in rat. The distribution of the nasally administered labeled micellar nanocarrier in various regions of the rat brain was determined using the brain localization and autoradiography studies. RESULTS:Micellar nanocarrier of zolmitriptan, with size of around 23 nm, was successfully formulated. The spherical nature of the nanocarrier was confirmed using DLS, SANS and cryo-TEM. Toxicity studies indicated the safety for administration in the nasal cavity. In vivo biodistribution studies indicated the superiority of the developed nanocarrier for brain targeting when compared with the intravenous and nasal solutions of the drug. Brain localization and autoradiography studies illustrated the distribution of the drug in various regions of the brain and revealed a possible nose-to-brain transport pathway for the labeled drug. CONCLUSION:The investigation indicated the potential of the developed nanocarrier as an effective new-generation vehicle for brain targeting of zolmitriptan.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Jain R,Nabar S,Dandekar P,Patravale Vdoi
10.1007/s11095-009-0041-xsubject
Has Abstractpub_date
2010-04-01 00:00:00pages
655-64issue
4eissn
0724-8741issn
1573-904Xjournal_volume
27pub_type
杂志文章abstract：PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9906-2
更新日期：2009-08-01 00:00:00
abstract：PURPOSE:One of the major hurdles facing nanomedicines is the antibody production against nanoparticles that subsequently results in their opsonization and clearance by macrophages. The objective of this research was to examine and identify the sequence of a low-immunogenic peptide based on recombinant elastin-like poly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1683-5
更新日期：2015-09-01 00:00:00
abstract：PURPOSE:The objective of this study was to compare two different nebulizers: Eflow rapid® and Pari LC star® by scintigraphy and PK modeling to simulate epithelial lining fluid concentrations from measured plasma concentrations, after nebulization of CMS in baboons. METHODS:Three baboons received CMS by IV infusion and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1716-0
更新日期：2015-10-01 00:00:00
abstract：PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1869-5
更新日期：2016-05-01 00:00:00
abstract：PURPOSE:To identify High Molecular Weight Products (HMWP) formed in human insulin formulation during storage. METHODS:Commercial formulation of human insulin was stored at 37°C for 1 year and HMWP was isolated using preparative size exclusion chromatography (SEC) and reverse phase (RP) chromatography. The primary stru...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1600-3
更新日期：2015-06-01 00:00:00
abstract：PURPOSE:The aim of the present study was to improve the dry powder inhalation behavior of steroid KSR-592 with lactose by altering the crystal shape and the particle size of the drug for use in a newly designed inhalation device, Jethaler. METHOD:The shape of the crystals was changed by polymorphic transformation of o...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1020492213172
更新日期：2002-10-01 00:00:00
abstract：PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The mor...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1568-z
更新日期：2015-05-01 00:00:00
abstract：PURPOSE:Some patients are unable to generate the peak inspiratory flow rate (PIFR) necessary to de-agglomerate drug particles from dry powder inhalers (DPIs). In this study we tested the hypothesis that the acoustic parameters of an inhalation are related to the PIFR and hence reflect drug delivery. METHODS:A sensitiv...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1371-x
更新日期：2014-10-01 00:00:00
abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0713-9
更新日期：2012-07-01 00:00:00
abstract：:Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secon...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015973425708
更新日期：1988-08-01 00:00:00
abstract：PURPOSE:To study the influence of cytotoxicity of macromolecules, VEGF gene expression, and vascular permeability on the enhanced permeability and retention (EPR) effect. METHODS:Mice bearing xenografts of A2780 multidrug resistant human ovarian carcinoma were treated by free doxorubicin (DOX) and N-(2-hydroxypropyl)m...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007500412442
更新日期：2000-05-01 00:00:00
abstract：:A method is described for the assay of phenobarbital N-glucosylation using UDP-D-[6-3H]glucose. The radioactive phenobarbital N-glucoside conjugates [(5R)-PBG, (5S)-PBG] formed during the incubations were resolved from each other and from uncharacterized radioactive products by semipreparative HPLC. The product ratio ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015889707922
更新日期：1992-05-01 00:00:00
abstract：PURPOSE:To assess the efficacy of lipid-protein-sugar particles (LPSPs) in providing prolonged duration local anesthesia by percutaneous injection. METHODS:Bupivacaine-containing LPSPs were characterized and optimized in vitro. Male Sprague-Dawley rats were given sciatic nerve blocks with bupivacaine-containing LPSPs....
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1026470831256
更新日期：2000-10-01 00:00:00
abstract：PURPOSE:To study the miscibility of proteins and polymer excipients in frozen solutions and freeze-dried solids as protein formulation models. METHODS:Thermal profiles of frozen solutions and freeze-dried solids containing various proteins (lysozyme, ovalbumin, BSA), nonionic polymers (Ficoll, polyvinylpyrrolidone [PV...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1026412107574
更新日期：2000-10-01 00:00:00
abstract：:Recently a new in vivo approach in man, using a regional intestinal perfusion technique, has been developed. The perfusion tube consists of a multichannel tube with two inflatable balloons, which are placed 10 cm apart. The tube is introduced orally and the time required for insertion and positioning of the tube is ap...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015888813741
更新日期：1992-10-01 00:00:00
abstract：PURPOSE:This study aims to develop a characterization method for coating structure based on image analysis, which is particularly promising for the rational design of coated particles in the pharmaceutical industry. METHODS:The method applies the MATLAB image processing toolbox to images of coated particles taken with...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9805-y
更新日期：2009-04-01 00:00:00
abstract：PURPOSE:To investigate the mechanisms involved in transport of sulfasalazine in Caco-2 cells. METHODS:Permeability coefficients of sulfasalazine and its analogs across Caco-2 cell monolayers were measured as a function of direction of transport, energy and concentration dependence, and in the presence of inhibitors of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1026450326712
更新日期：2000-10-01 00:00:00
abstract：:New generation vaccines, particularly those based on recombinant proteins and DNA, are likely to be less reactogenic than traditional vaccines but are also less immunogenic. Therefore, there is an urgent need for the development of new and improved vaccine adjuvants. Adjuvants can be broadly separated into two classes...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1016104910582
更新日期：2002-06-01 00:00:00
abstract：:The role of phosphatidylserine in the cellular and subcellular lung distribution of quinidine was investigated in rats, since quinidine was found to bind preferentially to phosphatidylserine. The concentration of phosphatidylserine in the cellular and subcellular fractions was determined after separation by two-dimens...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015985511653
更新日期：1988-04-01 00:00:00
abstract：PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007570030368
更新日期：2000-11-01 00:00:00
abstract：:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018900124257
更新日期：1994-10-01 00:00:00
abstract：PURPOSE:To identify the mechanism behind the unexpected bio-performance of two amorphous solid dispersions: BMS-A/PVP-VA and BMS-A/HPMC-AS. METHODS:Solubility of crystalline BMS-A in PVP-VA and HPMC-AS was measured by DSC. Drug-polymer interaction parameters were obtained by Flory-Huggins model fitting. Drug dissoluti...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0695-7
更新日期：2012-10-01 00:00:00
abstract：:The plasma concentration-time profiles and pharmacokinetics were characterized for nicotine and its major metabolite, cotinine, after multiple daily application of a nicotine user-activated transdermal therapeutic system (UATTS) to nine healthy smokers. The volunteers abstained from smoking 24 hr prior to and during t...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015810019076
更新日期：1991-03-01 00:00:00
abstract：:Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015982521706
更新日期：1989-12-01 00:00:00
abstract：PURPOSE:Heparin immobilized porous poly(D,L-lactic-co-glycolic acid) (PLGA) microspheres were prepared for sustained release of basic fibroblast growth factor (bFGF) to induce angiogenesis. MATERIALS AND METHODS:Porous PLGA microspheres having primary amine groups on the surface were prepared using an oil-in-water (O/...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9039-9
更新日期：2006-08-01 00:00:00
abstract：PURPOSE:Hydroxylation of the antidepressant and smoking deterrent drug bupropion is a clinically important bioactivation and elimination pathway. Bupropion hydroxylation is catalyzed selectively by cytochrome P4502B6 (CYP2B6). CYP2B6-catalyzed bupropion hydroxylation has been used as an in vitro and in vivo phenotypic ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9535-1
更新日期：2008-06-01 00:00:00
abstract：:Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from cap...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016283027139
更新日期：1995-02-01 00:00:00
abstract：PURPOSE:Polyesters with hydrophilic domains, i.e., poly(D,L-lactic-co-glycolic-co-hydroxymethyl glycolic acid) (PLGHMGA) and a multiblock copolymer of poly(ε-caprolactone)-PEG-poly(ε-caprolactone) and poly(L-lactide) ((PC-PEG-PC)-(PL)) are expected to cause less acylation of encapsulated peptides than fully hydrophobic...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1685-3
更新日期：2015-09-01 00:00:00
abstract：PURPOSE:To develop a novel bioadhesive polymer that protects peptide drugs from luminal degradation by aminopeptidase N and to evaluate the system in vitro on porcine mucosa. METHODS:EDTA was covalently bound to chitosan in order to combine the bioadhesive properties of the polymer with the well known capacity of EDTA...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012108118670
更新日期：1997-07-01 00:00:00
abstract：:This study utilized different statistical techniques to evaluate the reliability (internal consistency) and the discriminant validity of the most widely used measures of organizational commitment and intention to quit (the employing organization). Data were obtained from a national mail survey of members of the Americ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018930718979
更新日期：1994-01-01 00:00:00
