Nanosuspension for improving the bioavailability of a poorly soluble drug and screening of stabilizing agents to inhibit crystal growth.

Abstract:

:The purpose of this study was to develop a nanosuspension of a poorly soluble drug by nanomilling process using wet media milling to achieve superior in vitro dissolution and high in vivo exposure in pharmacokinetic studies. A promising nanosuspension was developed with Vitamin E TPGS based formulation with particle size in the nano range. Although the formulation showed significant improvement during in vitro dissolution and in vivo plasma level, probably due to the strong hydrophobic interaction between Vitamin TPGS and the drug molecule, crystal growth was observed during stability studies. A systematic study was done with different combinations of solubilizer/stabilizer system in order to obtain a more stable nanosuspension. Hydroxypropyl methylcellulose (HPMC 3 cps) was found to stabilize the nanosuspension by better surface coverage due to stronger interaction with the drug as compared to other stabilizers used in this study.

journal_name

Int J Pharm

authors

Ghosh I,Bose S,Vippagunta R,Harmon F

doi

10.1016/j.ijpharm.2011.02.051

subject

Has Abstract

pub_date

2011-05-16 00:00:00

pages

260-8

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(11)00186-4

journal_volume

409

pub_type

杂志文章
  • Cold flow of estradiol transdermal systems: influence of drug loss on the in vitro flux and drug transfer across human epidermis.

    abstract::The objective was to quantify drug loss due to cold flow (CF) in marketed estradiol transdermal drug delivery systems (TDDS), and study its influence on the in vitro flux and drug transfer across contacting skin. TDDS samples (products-A and B) were induced with CF at 25 and 32°C/60% RH by applying 1-kg force for 72h....

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.10.013

    authors: Krishnaiah YS,Yang Y,Hunt RL,Khan MA

    更新日期:2014-12-30 00:00:00

  • Development of a new method to characterize (SMBV) antigen formulations using surface plasmon resonance technology.

    abstract::Supra Molecular Biovectors (SMBV) are nanoparticles composed by a polysaccharidic core surrounded by a lipid bilayer. They are designed for drug delivery and vaccine and can be administrated by nasal route. The association rate and the stability of association between active principle (AP) or antigens (Ag) with SMBV c...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00227-2

    authors: Siguier JP,Major M,Balland O

    更新日期:2002-08-21 00:00:00

  • Determining the simultaneous presence of drug nanocrystals in drug-loaded polymeric nanocapsule aqueous suspensions: a relation between light scattering and drug content.

    abstract::The encapsulation of lipophilic drugs in polymeric nanoparticles can form simultaneously both polymeric nanoparticles and drug nanocrystals. The objective was to detect the presence of nanocrystals in the nanoparticle suspensions using a simple methodology, and to determine if the nanocrystals are formed during prepar...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.04.007

    authors: Pohlmann AR,Mezzalira G,Venturini Cde G,Cruz L,Bernardi A,Jäger E,Battastini AM,da Silveira NP,Guterres SS

    更新日期:2008-07-09 00:00:00

  • Effective melanoma cancer suppression by iontophoretic co-delivery of STAT3 siRNA and imatinib using gold nanoparticles.

    abstract::Co-delivery of chemotherapeutic agents improve anti-tumor efficacy and reduce cancer resistance. Here, we report development of layer-by-layer assembled gold nanoparticles (LbL-AuNP) containing anti-STAT3 siRNA and imatinib mesylate (IM) to treat melanoma. The combination treatment with STAT3 siRNA and IM in B16F10 me...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.03.087

    authors: Labala S,Jose A,Chawla SR,Khan MS,Bhatnagar S,Kulkarni OP,Venuganti VVK

    更新日期:2017-06-20 00:00:00

  • Sponges carrying self-microemulsifying drug delivery systems.

    abstract::Self-microemulsifying drug delivery systems (SMEDDS) increase the solubility of lipophilic drugs. One barrier to their wide application is their liquid nature. We report on a new method to solidify SMEDDS-their incorporation in sponges made from a hydrophilic natural polymer. Using different freeze-drying schemes, spo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.09.024

    authors: Josef E,Bianco-Peled H

    更新日期:2013-12-15 00:00:00

  • Novel applications of ubiquinone biopolymer nanocarriers for preventive and regenerative therapeutics: The Saccharomyces cerevisiae paradigm.

    abstract::Since the last decade, nanodispersed drug delivery systems gain increasingly more importance for therapeutic research fields. The forced transport to the centers of inflammation is supposed to take advantage as a novel strategic approach. Thus, the focus of this study was to investigate the applicability of ubiquinone...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.11.034

    authors: Hoennscheidt C,Margaritis A,Krull R

    更新日期:2015-01-15 00:00:00

  • Tocosome: Novel drug delivery system containing phospholipids and tocopheryl phosphates.

    abstract::The potential of two derivatives of vitamin E, i.e. α-tocopheryl phosphate (TP) and di-α-tocopheryl phosphate (T2P), for the protection and delivery of therapeutics is being investigated in our laboratory and some promising results have been obtained so far. Novel nanocarrier systems containing TP, T2P and different l...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.06.037

    authors: Mozafari MR,Javanmard R,Raji M

    更新日期:2017-08-07 00:00:00

  • Antibacterial activity of triclosan chitosan coated graft on hernia graft infection model.

    abstract::The use of mesh in hernia repair has become common, because of lower recurrence rate and simple application. Data from the meta-analysis and the multi-central studies support the use of meshes in hernia repair. One of the complications due to the hernia repair with mesh is the infection. The incidence range is between...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.05.059

    authors: Cakmak A,Cirpanli Y,Bilensoy E,Yorganci K,Caliş S,Saribaş Z,Kaynaroğlu V

    更新日期:2009-11-03 00:00:00

  • Improvement of cellular uptake, in vitro antitumor activity and sustained release profile with increased bioavailability from a nanoemulsion platform.

    abstract::Paclitaxel, a potential anticancer agent against solid tumors has been restricted from its oral use due to poor water solubility as well as Pgp efflux property. The present study was aimed to improve the oral bioavailability of paclitaxel through development of (o/w) nanoemulsion consisting of Capryol 90 as internal p...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.10.055

    authors: Choudhury H,Gorain B,Karmakar S,Biswas E,Dey G,Barik R,Mandal M,Pal TK

    更新日期:2014-01-02 00:00:00

  • Safe and effective interferon-beta gene therapy for the treatment of multiple sclerosis by regulating biological activity through the design of interferon-beta-galectin-9 fusion proteins.

    abstract::Multiple sclerosis (MS) is the most common demyelinating disease. Despite the historical use of interferon-beta (IFN-β) for the treatment of patients with MS, concerns exist regarding the side effects of IFN-β. In this study, we designed a series of novel IFN-β fusion proteins containing galectin-9 (gal-9), which exer...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.12.010

    authors: Hamana A,Takahashi Y,Tanioka A,Nishikawa M,Takakura Y

    更新日期:2018-01-30 00:00:00

  • Liposome-like nanocapsules of dual drug-tailed betaine for cancer therapy.

    abstract::A novel dual drug-tailed betaine conjugate amphiphile has been firstly synthesized in which the polar headgroup is derived from glycine betaine and the hydrophobic tails are chlorambucil molecules. The newly prepared conjugate undergoes self-assembly to form stable liposome-like nanocapsules as an effective carrier wi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.08.006

    authors: Fang S,Niu Y,Zhang W,Zhang Y,Yu L,Zhang Y,Li X

    更新日期:2015-09-30 00:00:00

  • Role of individual test samples in optimal solutions in pharmaceuticals predicted using a nonlinear response surface method.

    abstract::Establishing a method to evaluate the reliability of an optimal solution is an exciting challenge for the nonlinear response surface method. We reported previously that the bootstrap (BS) resampling technique and Kohonen's self-organizing map are promising tools for meeting this challenge. To understand the usefulness...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.06.013

    authors: Onuki Y,Kikuchi S,Yasuda A,Takayama K

    更新日期:2010-08-30 00:00:00

  • A tunable extruded 3D printing platform using thermo-sensitive pastes.

    abstract::Extruded 3D printing is emerging as an attractive fabrication technology in the field of personalized oral medicines. The objective of this study was to develop a tunable extruded 3D printing platform based on thermo-sensitive gelatin pastes to meet the needs of achieving different drug release characteristics with fl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119360

    authors: Yang Y,Wang X,Lin X,Xie L,Ivone R,Shen J,Yang G

    更新日期:2020-06-15 00:00:00

  • Preparation and characterization of two-phase melt systems of lidocaine.

    abstract::The melting point of lidocaine was significantly lowered when mixed with thymol and/or aqueous ethanol. Mixtures of lidocaine and thymol at ratios within the range of 30:70-70:30 (w:w) became homogeneous oils at 25 degrees C. In a pH 9.2 carbonate buffer containing 25% ethanol, lidocaine (5%, w:w) also liquefied at 25...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(01)00689-5

    authors: Kang L,Jun HW,Mani N

    更新日期:2001-07-03 00:00:00

  • Hydrodynamics-induced variability in the USP apparatus II dissolution test.

    abstract::The USP tablet dissolution test is an analytical tool used for the verification of drug release processes and formulation selection within the pharmaceutical industry. Given the strong impact of this test, it is surprising that operating conditions and testing devices have been selected empirically. In fact, the flow ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.08.003

    authors: Baxter JL,Kukura J,Muzzio FJ

    更新日期:2005-03-23 00:00:00

  • Surface modification of acetaminophen particles by atomic layer deposition.

    abstract::Active pharmaceutical ingredients (APIs) are predominantly organic solid powders. Due to their bulk properties many APIs require processing to improve pharmaceutical formulation and manufacturing in the preparation for various drug dosage forms. Improved powder flow and protection of the APIs are often anticipated cha...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.04.031

    authors: Kääriäinen TO,Kemell M,Vehkamäki M,Kääriäinen ML,Correia A,Santos HA,Bimbo LM,Hirvonen J,Hoppu P,George SM,Cameron DC,Ritala M,Leskelä M

    更新日期:2017-06-15 00:00:00

  • Nanocapsule@xerogel microparticles containing sodium diclofenac: a new strategy to control the release of drugs.

    abstract::The aim of this work was to evaluate the potentiality to control the drug release of a new architecture of microparticles organized at the nanoscopic scale by assembling polymeric nanocapsules at the surface of drug-loaded xerogels. Xerogel was prepared by sol-gel method using sodium diclofenac, as hydrophilic drug mo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.02.005

    authors: da Fonseca LS,Silveira RP,Deboni AM,Benvenutti EV,Costa TM,Guterres SS,Pohlmann AR

    更新日期:2008-06-24 00:00:00

  • Electrospun zein/eudragit nanofibers based dual drug delivery system for the simultaneous delivery of aceclofenac and pantoprazole.

    abstract::Electrospun composite zein/eudragit nanofibers were developed with an aim to deliver two different classes of drugs simultaneously that would restrict/compensate the adverse effects of non-steroidal anti-inflammatory drugs (NSAIDs). Co-administration of proton pump inhibitors is beneficial for patients consuming NSAID...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.07.075

    authors: Karthikeyan K,Guhathakarta S,Rajaram R,Korrapati PS

    更新日期:2012-11-15 00:00:00

  • Non-viral gene delivery carrier and its three-dimensional transfection system.

    abstract::An increasing number of non-viral vectors are being developed for the use of gene delivery nowadays, among which cationic polymers and lipoplexes receive most attention. Most of these researches are focused on how to increase the transfection efficiency of non-viral vectors as well as the reduction of toxicity. In thi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2009.11.006

    authors: He CX,Tabata Y,Gao JQ

    更新日期:2010-02-15 00:00:00

  • Process and formulation characterizations of the thermal adhesion granulation (TAG) process for improving granular properties.

    abstract::In this study, we demonstrate the feasibility of using the thermal adhesion granulation (TAG) method to improve granular properties for preparing highly compressible excipients as direct tabletting aids. The TAG method subjects a mixture containing excipients, such as microcrystalline cellulose (MCC), lactose, starch,...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.02.002

    authors: Lin HL,Ho HO,Chen CC,Yeh TS,Sheu MT

    更新日期:2008-06-05 00:00:00

  • The impact of channel fill level on internal forces during continuous twin screw wet granulation.

    abstract::The forces experienced by the particles inside a twin screw granulator (TSG) are one of the most difficult parameters to measure quantitatively. However, it is possible to perform accurately this measurement through the use of dye containing calibrated microencapsulated sensors (CAMES) whose rupture is directly depend...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2018.12.052

    authors: Mendez Torrecillas C,Gorringe LJ,Rajoub N,Robertson J,Elkes RG,Lamprou DA,Halbert GW

    更新日期:2019-03-10 00:00:00

  • Swelling, melting point reduction and solubility of PEG 1500 in supercritical CO2.

    abstract::The knowledge of the solubility of PEG 1500 as well as the swelling and melting point variation in supercritical CO(2) in a relatively high-pressure range is a necessary prerequisite to set-up pharmaceutical processes dealing with the polymer in the molten state. Experiments carried out in a pressurized view cell indi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.12.048

    authors: Pasquali I,Comi L,Pucciarelli F,Bettini R

    更新日期:2008-05-22 00:00:00

  • Targeting energy metabolism of cancer cells: Combined administration of NCL-240 and 2-DG.

    abstract::Cancer cells increase their metabolism to produce the energy and biomolecules necessary for growth and proliferation. Thus, energy metabolism pathways may serve as targets for anti-cancer therapy. NCL-240 is a second generation anti-cancer drug belonging to the PITenins class of PI3K-Akt inhibitors. Our analysis sugge...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.08.095

    authors: Pattni BS,Jhaveri A,Dutta I,Baleja JD,Degterev A,Torchilin V

    更新日期:2017-10-30 00:00:00

  • Preparation, formula optimization and antitumor actions of mannitol coupling camptothecin nanoparticles.

    abstract::The purpose of this work is to prepare a formulation using mannitol coupling Camptothecin (CPT) nanoparticles (CPT-NPs) to circumvent the difficult solubilization practice based on central composite experimental statistical design. CPT-NPs were prepared with a high-pressure homogenization technique method. The indepen...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.02.019

    authors: Wang Z,Li Q,Zhao X,Sun B,Zhu Q,Gao W,Hua C

    更新日期:2014-04-25 00:00:00

  • Cell uptake, cytoplasmic diffusion and nuclear access of a 6.5 nm diameter dendrimer.

    abstract::Macromolecular crowding and the presence of organelles in the cytosol present barriers to particle mobility, such that it is unclear how nano-carriers can deliver their active agents to the nucleus. In this work a sixth generation amino terminated polyamide polylysine dendrimer (Gly-Lys(63) (NH(2))(64)) (MW 8149, diam...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.12.012

    authors: Ruenraroengsak P,Al-Jamal KT,Hartell N,Braeckmans K,De Smedt SC,Florence AT

    更新日期:2007-03-01 00:00:00

  • The breakage behaviour of Aspirin under quasi-static indentation and single particle impact loading: effect of crystallographic anisotropy.

    abstract::The influence of crystallographic structural anisotropy on the breakage behaviour of Aspirin under impact loading is highlighted. Under both quasi-static testing conditions, using nano-indentation, and dynamic impact tests, Aspirin demonstrates clear anisotropy in its slip and fracture behaviour. During nano-indentati...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.03.039

    authors: Olusanmi D,Roberts KJ,Ghadiri M,Ding Y

    更新日期:2011-06-15 00:00:00

  • Liposomal andrographolide dry powder inhalers for treatment of bacterial pneumonia via anti-inflammatory pathway.

    abstract::Andrographolide (AG) is a chemical entity from traditional Chinese herbs and its oral pills have been applied to the treatment of respiratory inflammation. Here we report pulmonary delivery of liposomal AG dry powder inhalers (LADPIs) for treatment of Staphylococcus aureus-induced pneumonia. AG liposomes were prepared...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.06.005

    authors: Li M,Zhang T,Zhu L,Wang R,Jin Y

    更新日期:2017-08-07 00:00:00

  • Bovine serum albumin-meloxicam nanoaggregates laden contact lenses for ophthalmic drug delivery in treatment of postcataract endophthalmitis.

    abstract::Postcataract endophthalmitis treatment through eye drops is of low corneal bioavailability and short residence time. The dominant NSAIDs therapy also suffers from severe ocular irritancy and low patients compliance. This study dispersed bovine serum albumin (BSA) coated meloxicam (MX) nanocrystals encapsulating nanoag...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.08.043

    authors: Zhang W,Zu D,Chen J,Peng J,Liu Y,Zhang H,Li S,Pan W

    更新日期:2014-11-20 00:00:00

  • Insulin nanoparticle preparation and encapsulation into poly(lactic-co-glycolic acid) microspheres by using an anhydrous system.

    abstract::Insulin has been encapsulated in poly(lactic-co-glycolic acid) (PLGA) microspheres by solid-in-oil-in-oil (S/O/O) emulsion technique using DMF/corn oil as new solvent pairs. To get better encapsulation efficiency, insulin nanoparticles were prepared by the modified isoelectric point precipitation method so that it had...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.05.021

    authors: Han Y,Tian H,He P,Chen X,Jing X

    更新日期:2009-08-13 00:00:00

  • Preparation and characterization of a synthetic curcumin analog inclusion complex and preliminary evaluation of in vitro antileishmanial activity.

    abstract::The aim of this work was to prepare and characterize inclusion complexes between a synthetic curcumin analog (dibenzalacetone, DBA) and beta-cyclodextrin (β-CD); and to evaluate their in vitro antileishmanial activity. DBA was synthetized and characterized by spectroscopic methods and the inclusion complexes were obta...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119764

    authors: Pinto LMA,Adeoye O,Thomasi SS,Francisco AP,Carvalheiro MC,Cabral-Marques H

    更新日期:2020-08-25 00:00:00