In vitro and in vivo evaluation of a hydrogel-based prototype transdermal patch system of alfuzosin hydrochloride.

Abstract:

:The first-line therapy for moderate to severe benign prostatic hyperplasia is the oral therapy by alfuzosin hydrochloride. Unfortunately, the oral therapy of alfuzosin is associated with several route-specific systemic side-effects. The current study was aimed to develop a prototype transdermal patch system for alfuzosin using a hydrogel polymer and optimize the drug delivery through the skin for systemic therapy. The prospective of different chemical enhancers (polyethylene glycol (PEG 400), isopropyl myristate, propylene glycol, menthol and L-methionine; 5% w/v) and iontophoresis (0.3 mA/cm(2)) in the alfuzosin delivery across the full thickness rat skin was assessed in vitro. In vivo iontophoretic studies were carried out using selected patch system (PEG 400) for a period of 6 h in Sprague-Dawley rats. Passive permeation studies indicated that the incorporation of chemical agents have moderate effect (~4- to 7-fold) on the alfuzosin skin permeability and reduced the lag time. Combined approach of iontophoresis with chemical enhancers significantly augmented the drug transport (~ 43- to 72-fold). In vivo pharmacokinetic parameters revealed that the iontophoresis (transdermal patch with PEG 400) significantly enhanced the C(max) (~ 3-fold) and AUC(0-α) (~ 4-fold), when compared to control. The current study concludes that the application of iontophoresis (0.3 mA/cm(2)) using the newly developed agaorse-based prototype patch with PEG 400 could be utilized for the successful delivery of alfuzosin by transdermal route.

journal_name

Pharm Dev Technol

authors

Nair AB,Vaka SR,Gupta S,Repka MA,Murthy SN

doi

10.3109/10837450.2010.522585

subject

Has Abstract

pub_date

2012-03-01 00:00:00

pages

158-63

issue

2

eissn

1083-7450

issn

1097-9867

journal_volume

17

pub_type

杂志文章
  • Comparison of various injectable protein-loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices: in-situ-formed implant versus in-situ-formed microspheres versus isolated microspheres.

    abstract::The purpose of this research was to prepare various injectable, protein (cytochrome c)-loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices by a novel microencapsulation method and to compare their characteristics. Syringeable mixtures of polymer and protein solidified upon injection when coming in contact w...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100100535

    authors: Jain RA,Rhodes CT,Railkar AM,Malick AW,Shah NH

    更新日期:2000-01-01 00:00:00

  • Polymorphism and solvates of flecainide base.

    abstract::Flecainide base is pharmaceutically active substance used for production of flecainide acetate which is known in market as Tambacor, Almarytm, Apocard, Ecrinal or Flecaine. It is determined that flecainide base forms four polymorphic forms abbreviated as Ib, IIb, IIIb and IVb. Flecainide base form Ib is thermodynamica...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.763259

    authors: Veldre K,Eglīte Z,Actiņš A,Zvirgzdiņš A,Rozenberga L,Tamanis E

    更新日期:2014-02-01 00:00:00

  • Gastroretentive bilayer film for sustained release of atorvastatin calcium and immediate release of amlodipine besylate: pharmaceutical, pharmacokinetic evaluation, and IVIVC.

    abstract::The present study was aimed to optimize capsulated unfolding type gastroretentive bilayer film constituting immediate release (IR) layer of amlodipine besylate and sustained release (SR) layer of atorvastatin calcium. A three-factor, three-level Box-Behnken-design was used to optimize bilayer film with dual-release ch...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1705486

    authors: Porwal A,Dwivedi H,Pathak K

    更新日期:2020-04-01 00:00:00

  • One-step preparation of ibuprofen fast- and sustained-release formulation by electrospinning with improved efficacy and reduced side effect.

    abstract::In this study, we developed a one-step method to prepare ibuprofen fast- and sustained-release complex preparation. It was based on a double jets electrospinning process. Ibuprofen, a poorly water-soluble drug, was electrospun into fibers with polyvinyl pyrrolidone and hydroxypropyl methyl cellulose by two jets, respe...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1728773

    authors: Che X,Xue J,Zhang J,Yang X,Wang L

    更新日期:2020-07-01 00:00:00

  • Construction and cellular uptake behavior of redox-sensitive docetaxel prodrug-loaded liposomes.

    abstract::A redox-responsive docetaxel (DTX) prodrug consisting of a disulfide linkage between DTX and vitamin E (DTX-SS-VE) was synthesized in our laboratory and was successfully formulated into liposomes. The aim of this study was to optimize the formulation and investigate the cellular uptake of DTX prodrug-loaded liposomes ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1287728

    authors: Ren G,Jiang M,Guo W,Sun B,Lian H,Wang Y,He Z

    更新日期:2018-01-01 00:00:00

  • The development and in vitro evaluation of herbal pellets coated with Eudragit FS 30.

    abstract::The objective of this study was to prepare pellets of thyme (Thymus vulgaris L.), stinging nettle (Urtica dioica L.) and sage (Salvia officinalis L.) dry extracts by extrusion-spheronization technique to improve technological properties and investigate dissolution profiles of pellets covered different levels of pH-sen...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.920355

    authors: Kaledaite R,Bernatoniene J,Dvořáčková K,Gajdziok J,Muselík J,Pečiūra R,Masteikova R

    更新日期:2015-11-01 00:00:00

  • Complexation and solubility behavior of albendazole with some cyclodextrins.

    abstract::The main purpose of this work was to study the albendazole-cyclodextrins complexation equilibrium and to propose a suitable excipient to improve the solubility behavior and dissolution rate of albendazole. The complexation of albendazole with four cyclodextrins, alpha-CD, beta-CD, gamma-CD, and hydroxypropylated (HP)-...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459809009867

    authors: Díaz D,Bernad Bernad MJ,Gracia Mora J,Escobar Llanos CM

    更新日期:1998-08-01 00:00:00

  • Use of poloxamer polymers to stabilize recombinant human growth hormone against various processing stresses.

    abstract::Several processing and shipping stresses were investigated for their effect on the physical stability of recombinant human growth hormone (rhGH). These included exposure to air/water interfaces, adsorption to hydrophobic surfaces, freeze-thaw cycles, and temperature. The interfacially and thermally denatured hormone w...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459709022619

    authors: Katakam M,Banga AK

    更新日期:1997-05-01 00:00:00

  • Mechanoradical-induced degradation in a pharmaceutical blend during high-shear processing.

    abstract::Mechanically generated radicals were shown to affect short-term stability of a model pharmaceutical formulation during high-shear processing. A formulation containing an oxidatively sensitive drug, either amorphous or crystalline, and a polymeric excipient was high-shear mixed and the resulting short-term degradation ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802328869

    authors: Polizzi MA,Singhal D,Colvin J

    更新日期:2008-01-01 00:00:00

  • Coprocessing of nevirapine and stavudine by spray drying.

    abstract::The objective of the present study was to coprocess 2 active pharmaceutical ingredients (APIs), nevirapine (NVP) and stavudine (STV), by spray drying technique to overcome the respective problems of poor solubility and poor content uniformity. The coprocessed product (NVP-STV CP) and untreated APIs were characterized ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802089164

    authors: Mohammed GA,Puri V,Bansal AK

    更新日期:2008-01-01 00:00:00

  • Controlled delivery of the antiprotozoal agent (tinidazole) from intravaginal polymer matrices for treatment of the sexually transmitted infection, trichomoniasis.

    abstract::Microporous polymeric matrices prepared from poly(ɛ-caprolactone) [PCL] were evaluated for controlled vaginal delivery of the antiprotozoal agent (tinidazole) in the treatment of the sexually transmitted infection, trichomoniasis. The matrices were produced by rapidly cooling co-solutions of PCL and tinidazole in acet...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1481430

    authors: Fernando HV,Chan LL,Dang N,Santhanes D,Banneheke H,Nalliah S,Coombes AGA

    更新日期:2019-03-01 00:00:00

  • Prolonged injectable formulation of Nafarelin using in situ gel combination delivery system.

    abstract::The principal purpose of the present study was to prepare and characterize a complex drug delivery system consisting of Nafarelin-poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanoparticles (NPs) in combination with sodium alginate/poloxamer 407 in situ gel. Nafarelin-loaded PHBV NPs were prepared via double em...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1321662

    authors: Alizadeh B,Bahari Javan N,Akbari Javar H,Khoshayand MR,Dorkoosh F

    更新日期:2018-02-01 00:00:00

  • Fabrication and evaluation of Phytomenadione as a nanostructure lipid carrier for enhancement of bioavailability.

    abstract::Owing to its limited aqueous solubility, Phytomenadione (vitamin K) undergoes a low bioavailability (50%) with a large inter-individual variability after oral administration. Therefore, the aim of this work was to incorporate vitamin K into nanostructure lipid carrier systems to improve its aqueous solubility and bioa...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1312440

    authors: Aljaeid BM,Hosny KM

    更新日期:2018-04-01 00:00:00

  • Doxorubicin-loaded microgels composed of cinnamic acid-gelatin conjugate and cinnamic acid-Pluronic F127 conjugate.

    abstract::Microgels were prepared by cinnamic acid-gelatin (type B) conjugate (CA-GelB) and cinnamic acid-Pluronic F127 conjugate (CA-Plur). (1)H NMR confirmed that CA was conjugated to gelatin and the gelatin to CA residue molar ratio was estimated to be 1:4.7 by a colorimetric method. CA-Plur of which the CA residue to Plur m...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.999787

    authors: Zhang H,Kim JC

    更新日期:2016-01-01 00:00:00

  • Design and evaluation of ocular drug delivery system for controlled delivery of gatifloxacin sesquehydrate: In vitro and in vivo evaluation.

    abstract::The objective of this investigation was to formulate ocular inserts of gatifloxacin sesquehydrate to achieve controlled drug release. Drug reservoir was prepared using hydrophilic polymers, namely polyvinyl alcohol and polyvinyl pyrrolidone. The rate controlling membrane was prepared using hydrophobic ethyl cellulose ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.502178

    authors: Patel UL,Chotai NP,Nagda CD

    更新日期:2012-01-01 00:00:00

  • In vitro/in vivo correlation and modeling of emitted dose and lung deposition of inhaled salbutamol from metered dose inhalers with different types of spacers in noninvasively ventilated patients.

    abstract::Substituting spacer by another in noninvasive ventilation (NIV) involves many variables, e.g. total emitted dose (TED), mass median aerodynamic diameter (MMAD), type of spacer, total lung deposition and total systemic absorption, which must be adjusted to ensure patient optimum therapy. Data mining based on artificial...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1116567

    authors: Hussein RRS,M A Ali A,Salem HF,Abdelrahman MM,Said ASA,Abdelrahim MEA

    更新日期:2017-11-01 00:00:00

  • Controlled release of DSBP from genipin-crosslinked gelatin thin films.

    abstract::Controlled release of a marker drug, 4,4'-bis(2-sulfostyryl) biphenyl (DSBP) from genipin crosslinked gelatin thin films, with application to drug delivery by transdermal patches is studied in this paper. A simple method for fabrication of nano-thin films, using basic lab equipment is introduced. This method consists ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802309679

    authors: Abbasi A,Eslamian M,Heyd D,Rousseau D

    更新日期:2008-01-01 00:00:00

  • Multiunit controlled-release diclofenac sodium capsules using complex of chitosan with sodium alginate or pectin.

    abstract::This study explored the application of chitosan-alginate (CA) and chitosan-pectin (CP) complex films as drug release regulator for the preparation of multiunit controlled-release diclofenac sodium capsules. Pellets containing drug and microcrystalline cellulose, in a ratio of 3:5, were prepared in a fluidized rotary g...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100002247

    authors: Mitrevej A,Sinchaipanid N,Rungvejhavuttivittaya Y,Kositchaiyong V

    更新日期:2001-08-01 00:00:00

  • Photoinduced particulate matter in a parenteral formulation for bisnafide, an experimental antitumor agent.

    abstract::This paper assesses the cause of particulate formation in vials of the experimental antitumor agent bisnafide and investigates pharmaceutical techniques to reduce the number of particulates in the product. Solution preparation and particulate isolation were performed under Class 100 laminar air flow. Reversed-phase HP...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100101380

    authors: Rubino JT,Chan LL,Walker JT,Segretario J,Everlof JG,Hussain MA

    更新日期:1999-08-01 00:00:00

  • Nano drug delivery systems and gamma radiation sterilization.

    abstract::In recent years, drug delivery systems such as liposomes and microparticles have been used in clinic for the treatment of different diseases and from a regulatory point of view, a parenterally applied drug and drug delivery systems must be sterile and pyrogen free. Radiation sterilization is a method recognized by pha...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2016.1163393

    authors: Sakar F,Özer AY,Erdogan S,Ekizoglu M,Kart D,Özalp M,Colak S,Zencir Y

    更新日期:2017-09-01 00:00:00

  • Iontophoretic enhancement of leuprolide acetate by fatty acids, limonene, and depilatory lotions through porcine epidermis.

    abstract::The effect of chemical enhancers (e.g., fatty acids, limonene, depilatory lotions) and iontophoresis was investigated on the in vitro permeability of leuprolide acetate through porcine epidermis. Franz diffusion cells and Scepter iontophoretic power source were used for the percutaneous absorption studies. Anodal iont...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-200032986

    authors: Rastogi SK,Singh J

    更新日期:2004-11-01 00:00:00

  • Enhancement of the intestinal absorption of bortezomib by self-nanoemulsifying drug delivery system.

    abstract::Purpose: Intestinal drug absorption is one of the main factors that govern the fraction of oral dose absorbed (Fa) of drugs. It is reported that oral absorption of bortezomib (BTZ) can be restricted by its low intestinal permeability. In this study, we aimed to evaluate the impact of self-nanoemulsifying drug delivery...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1699109

    authors: Mahmoudian M,Valizadeh H,Löbenberg R,Zakeri-Milani P

    更新日期:2020-03-01 00:00:00

  • Identification of physical-chemical variables affecting particle size following precipitation using a supercritical fluid.

    abstract::The physical-chemical processing variables affecting particle size following precipitation using the supercritical antisolvent (SAS) method were investigated by varying both the composition of the feed solvent and the structure of the solute, using a series of steroids. The key factor influencing particle size in thes...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450600561299

    authors: Sacha GA,Schmitt WJ,Nail SL

    更新日期:2006-01-01 00:00:00

  • Preparation and in vitro characterization of diltiazem hydrochloride loaded alginate microspheres.

    abstract::The main objective of the present study was to improve bioavailability of diltiazem hydrochloride and decrease the frequency of dosage form administration by increasing the encapsulation efficiency of the drug, residence time of the dosage form at the site of absorption and sustained release of the drug from the deliv...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802626304

    authors: Sultana Y,Mall S,Maurya DP,Kumar D,Das M

    更新日期:2009-01-01 00:00:00

  • Properties of bioadhesive ketoprofen liquid suppositories: preparation, determination of gelation temperature, viscosity studies and evaluation of mechanical properties using texture analyzer by 4 × 4 factorial design.

    abstract:CONTEXT:Development and evaluation of thermosensitive and bioadhesive liquid suppositories containing ketoprofen (KP). OBJECTIVE:This study was conducted to develope thermosensitive and bioadhesive liquid suppositories containing KP using poloxamer and different bioadhesive polymers and to investigate their gelation t...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.846373

    authors: Ozgüney I,Kardhiqi A

    更新日期:2014-12-01 00:00:00

  • PLGA-PEG-RA-based polymeric micelles for tumor targeted delivery of irinotecan.

    abstract::To develop an effective therapeutic treatment, the potential of poly (lactic-co-glycolic acid)-polyethylene glycol-retinoic acid (PLGA-PEG-RA) polymeric micelles for targeted delivery of irinotecan to hepatocellular carcinoma (HepG2) and colorectal cancer cell lines (HT-29) was evaluated. PLGA-PEG-RA was synthesized b...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1340950

    authors: Emami J,Maghzi P,Hasanzadeh F,Sadeghi H,Mirian M,Rostami M

    更新日期:2018-01-01 00:00:00

  • Preparation of meloxicam-β-cyclodextrin-polyethylene glycol 6000 ternary system: characterization, in vitro and in vivo bioavailability.

    abstract::Ternary complexes of meloxicam (ML), a poorly water-soluble anti-inflammatory drug, with β-cyclodextrin (βCD) and polyethylene glycol (PEG) 6000 were prepared from an equimolar (ML-βCD) and 10% of PEG. Characterization of the ternary complex was carried out by differential scanning calorimetry and X-ray diffractometry...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2011.565347

    authors: Radia O,Rogalska E,Moulay-Hassane G

    更新日期:2012-09-01 00:00:00

  • Polyacrylic acid polymers hydrogels intended to topical drug delivery: preparation and characterization.

    abstract:CONTEXT:Bioadhesiviness of polyacrylic acid polymers make them promising hydrogels to design topical drug delivery systems, allowing a close contact with biological substrate as well as an enhanced local concentration gradient, both factors that may improve the biological performance of the drugs. AIM:Texture and bioa...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.882941

    authors: Calixto G,Yoshii AC,Rocha e Silva H,Stringhetti Ferreira Cury B,Chorilli M

    更新日期:2015-06-01 00:00:00

  • Influence of the type of vegetable oil on the drug release profile from lipid-core nanocapsules and in vivo genotoxicity study.

    abstract::The use of rice bran (RB), soybean (SB) or sunflower seed (SF) oils to prepare lipid-core nanocapsules (LNCs) as controlled drug delivery systems was investigated. LNCs were prepared by interfacial deposition using the preformed polymer method. All formulations showed negative zeta potential and adequate nanotechnolog...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.829097

    authors: Rigo LA,Frescura V,Fiel L,Coradini K,Ourique AF,Emanuelli T,Quatrin A,Tedesco S,Silva CB,Guterres SS,Pohlmann AR,Beck RC

    更新日期:2014-11-01 00:00:00

  • Encapsulation of plai oil/2-hydroxypropyl-β-cyclodextrin inclusion complexes in polyvinylpyrrolidone (PVP) electrospun nanofibers for topical application.

    abstract::The aim of this study was to prepare electrospun polyvinylpyrrolidone (PVP)/2-hydroxypropyl-β-cyclodextrin (HPβCD) nanofiber mats and to incorporate plai oil (Zingiber Cassumunar Roxb.). The plai oil with 10, 20 and 30% wt to polymer were incorporated in the PVP/HPβCD solution and electrospun to obtain nanofibers. The...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.788659

    authors: Tonglairoum P,Chuchote T,Ngawhirunpat T,Rojanarata T,Opanasopit P

    更新日期:2014-06-01 00:00:00