Alginate-Based Delivery Systems for Bevacizumab Local Therapy: In Vitro Structural Features and Release Properties.

Abstract:

:Alginate-based polyelectrolyte complexes (PECs) and hydrogel were engineered as platforms for local bevacizumab (BVZ) therapy. This study provides deep comprehension on the microstructures of such systems, and their correlation with drug-release patterns. PECs and hydrogel were characterized using Fourier transform infrared spectroscopy, small-angle X-ray scattering, scanning electron microscopy, atomic force microscopy, and porosimetry. Structural investigations indicated that PECs are formed by supramolecular interactions, resulting in physically cross-linked polymer networks, whereas the BVZ-loaded hydrogel has a more compact and rigid structure, promoting better entrapment of BVZ. PECs and hydrogel were able to control the BVZ release for 4 and 8 days, respectively. Their release profiles correlated best with the Higuchi and Korsmeyer-Peppas models, respectively, indicating drug diffusion as the limiting step for drug release. Furthermore, BVZ remained biologically active in vitro after its incorporation into the hydrogel system. Together, these studies confirm that PECs and hydrogel exhibit different porous structures and physicochemical properties, making them promising platforms that allow the modulation of BVZ release meeting different requirements.

journal_name

J Pharm Sci

authors

Ferreira NN,Caetano BL,Boni FI,Sousa F,Magnani M,Sarmento B,Ferreira Cury BS,Daflon Gremião MP

doi

10.1016/j.xphs.2018.11.038

subject

Has Abstract

pub_date

2019-04-01 00:00:00

pages

1559-1568

issue

4

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(18)30786-X

journal_volume

108

pub_type

杂志文章
  • Prediction of the relaxation behavior of amorphous pharmaceutical compounds. I. Master curves concept and practice.

    abstract::Variability in the time to crystallization is a major technical and economic hurdle in using amorphous solids in dosage forms. It is hypothesized that amorphous solids "age", and that the older they are, the more relaxed they are and the higher the probability of crystallization. At present, there is no method that al...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10404

    authors: Hilden LR,Morris KR

    更新日期:2003-07-01 00:00:00

  • Effect of repeated skin application on percutaneous absorption of salicylic acid.

    abstract::Various concentrations of salicylic acid in hydrophilic ointment were applied repeatedly at daily or weekly intervals to rats in vivo. Salicylic acid absorption through treated skin was monitored by determining the penetration fluxes of salicylic acid through skin excised at various times. A gradual decrease in the sa...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600671213

    authors: Roberts MS,Harlock E

    更新日期:1978-12-01 00:00:00

  • Colorimetric determination of nadolol in tablets.

    abstract::Nadolol was extracted from tablet excipients with an acidic potassium chloride solution. The drug was oxidized with periodic acid, and the resulting aldehyde was reacted with 2,4-dinitrophenylhydrazine to form the corresponding hydrazone. Excess reagent was removed with a cupric chloride solution. The hydrazone was ex...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670743

    authors: Ivashikiv E

    更新日期:1978-07-01 00:00:00

  • Solid and Solution State Thermodynamics of Polymorphs of Butamben (Butyl 4-Aminobenzoate) in Pure Organic Solvents.

    abstract::The solubility of butamben has been measured gravimetrically in pure methanol, 1-propanol, 2-propanol, 1-butanol, and toluene over the temperature range 268-298 K. Polymorph transition and melting temperatures, associated enthalpy changes, and the heat capacity of the solid forms and the supercooled melt have been mea...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.02.013

    authors: Svärd M,Zeng L,Valavi M,Krishna GR,Rasmuson ÅC

    更新日期:2019-07-01 00:00:00

  • A theoretical model for transdermal drug delivery from emulsions and its dependence upon formulation.

    abstract::This article presents a theoretical model of transdermal drug delivery from an emulsion-type vehicle that addresses the vehicle heterogeneity and incorporates the prediction of drug transport parameters as function of the vehicle composition. The basic mass transfer model considers interfacial and diffusion resistance...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21268

    authors: Bernardo FP,Saraiva PM

    更新日期:2008-09-01 00:00:00

  • Finding the Needle in the Haystack: High-Resolution Techniques for Characterization of Mixed Protein Particles Containing Shed Silicone Rubber Particles Generated During Pumping.

    abstract::During the manufacturing process of biopharmaceuticals, peristaltic pumps are employed at different stages for transferring and dosing of the final product. Commonly used silicone tubings are known for particle shedding from the inner tubing surface due to friction in the pump head. These nanometer sized silicone rubb...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.12.002

    authors: Deiringer N,Haase C,Wieland K,Zahler S,Haisch C,Friess W

    更新日期:2020-12-09 00:00:00

  • Characterization of glucose-mediated insulin release from implantable polymers.

    abstract::We characterized a glucose-sensitive, controlled-release insulin delivery system. Insulin release rates increased when glucose was perfused in the release media surrounding the matrix. The system was composed of solid, particulate insulin, incorporated into an ethylene-vinyl acetate copolymer (EVAc) matrix. Feedback c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9600686

    authors: Brown LR,Edelman ER,Fischel-Ghodsian F,Langer R

    更新日期:1996-12-01 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

  • Synthesis and evaluation of N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine as a colon-specific prodrug of metronidazole.

    abstract::Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21720

    authors: Kim D,Hong S,Jung S,Jung Y,Kim YM

    更新日期:2009-11-01 00:00:00

  • The granule porosity controls the loss of compactibility for both dry- and wet-processed cellulose granules but at different rate.

    abstract::The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the comp...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24439

    authors: Nordström J,Alderborn G

    更新日期:2015-06-01 00:00:00

  • The use of 13C labeling to enhance the sensitivity of 13C solid-state CPMAS NMR to study polymorphism in low dose solid formulations.

    abstract::(13)C labeling was used to enhance the sensitivity of (13)C solid-state NMR to study the effect of tabletting on the polymorphism of a steroidal drug. The steroidal drug Org OD 14 was (13)C labeled and formulated into tablets containing only 0.5-2.5% active ingredient. The tablets were subsequently studied by solid-st...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20236

    authors: Booy KJ,Wiegerinck P,Vader J,Kaspersen F,Lambregts D,Vromans H,Kellenbach E

    更新日期:2005-02-01 00:00:00

  • Spray-freeze-drying for protein powder preparation: particle characterization and a case study with trypsinogen stability.

    abstract::This work investigates the use of spray freeze-drying (SFD) to produce protein loaded particles suitable for epidermal delivery. In the first part of the study, the effects of formulation and process conditions on particle properties are examined. Aqueous solutions of trehalose produce SFD particles in the size range ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10204

    authors: Sonner C,Maa YF,Lee G

    更新日期:2002-10-01 00:00:00

  • Development of a Rational Design Space for Optimizing Mixing Conditions for Formation of Adhesive Mixtures for Dry-Powder Inhaler Formulations.

    abstract::The purpose of the present study was to develop guidance toward rational choice of blenders and processing conditions to make robust and high performing adhesive mixtures for dry-powder inhalers and to develop quantitative experimental approaches for optimizing the process. Mixing behavior of carrier (LH100) and Astra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.07.012

    authors: Sarkar S,Minatovicz B,Thalberg K,Chaudhuri B

    更新日期:2017-01-01 00:00:00

  • The future of protein particle characterization and understanding its potential to diminish the immunogenicity of biopharmaceuticals: a shared perspective.

    abstract::Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23247

    authors: Bee JS,Goletz TJ,Ragheb JA

    更新日期:2012-10-01 00:00:00

  • Partial molal volumes and solubilities of physostigmine in isopropanol:isopropyl myristate solvents in relation to skin penetrability.

    abstract::Partial molal volumes (Vi infinity) of physostigmine, ranging from 232.9 to 239.8 cm3.mol-1, and its mole fraction solubilities (Xi), ranging from 0.051 to 0.009, were determined at 25 degrees C in solutions of isopropanol (IPA), isopropyl myristate (IPM), and their mixtures. An inverse relation was found between Vi i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600800615

    authors: Pardo A,Shiri Y,Cohen S

    更新日期:1991-06-01 00:00:00

  • Degradation kinetics of phentolamine hydrochloride in solution.

    abstract::The degradation kinetics of phentolamine hydrochloride in aqueous solution over a pH range of 1.2 to 7.2 and its stability in propylene glycol- or polyethylene glycol 400-based solutions were investigated. The observed rate constants were shown to follow apparent first-order kinetics in all cases. The pKa determinatio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600771116

    authors: Wang DP,Tu YH,Allen LV Jr

    更新日期:1988-11-01 00:00:00

  • Polymeric systems for amorphous Delta 9-tetrahydrocannabinol produced by a hot-melt method. Part I: chemical and thermal stability during processing.

    abstract::The objective of the present research was to investigate the stability of an amorphous drug, Delta(9)-tetrahydrocannabinol (THC) in polymer-based transmucosal systems. THC was incorporated in polyethylene oxide and hydroxypropylcellulose matrices by a hot-melt fabrication procedure, utilizing various processing aids. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20667

    authors: Munjal M,Stodghill SP,Elsohly MA,Repka MA

    更新日期:2006-08-01 00:00:00

  • Usefulness of PBPK Modeling in Incorporation of Clinical Conditions in Personalized Medicine.

    abstract::Personalized medicine aims to determine the most adequate treatment and dose regimen to obtain the maximum efficacy and minimum side effect by taking into account patients' characteristics. For numerous reasons, one being ethical and methodological hurdles in including specific populations in clinical trials, innovati...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2017.04.035

    authors: Marsousi N,Desmeules JA,Rudaz S,Daali Y

    更新日期:2017-09-01 00:00:00

  • In Vitro and In Vivo Studies of Polyvinyl Pyrrolidone-Coated Sparfloxacin-Loaded Ring Contact Lens to Treat Conjunctivitis.

    abstract::Currently, conjunctivitis is treated by frequent high dose administration of sparfloxacin eye drop solution. However, the eye drops are inconvenient because of low bioavailability, short ocular drug residence time, and need of frequent instillation, which lead to patient noncompliance affecting the routine life style ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.02.008

    authors: Ran W,Ma H,Li M

    更新日期:2020-06-01 00:00:00

  • Injectable polyanhydride granules provide controlled release of water-soluble drugs with a reduced initial burst.

    abstract::A method for preparing polyanhydride granules of an injectable size was developed. The resulting granules permitted a nearly constant release of low-molecular-weight, water-soluble drugs without an initial burst. The polyanhydrides used were poly(fatty acid dimer), poly(sebacic acid), and their copolymers. The dyes ac...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600830104

    authors: Tabata Y,Domb A,Langer R

    更新日期:1994-01-01 00:00:00

  • Kinetics and mechanism of oxidation of promazine and promethazine by ferric perchlorate.

    abstract::The equilibrium constants, kinetics, and mechanism of promazine and promethazine oxidation by ferric perchlorate were investigated at different temperatures and acidities using a stopped-flow spectrophotometric technique. The overall reaction can be represented as follows: (formula: see text) where P+ represents the r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670212

    authors: Gasco MR,Carlotti ME

    更新日期:1978-02-01 00:00:00

  • Correlation between chemical reactivity and the Hammett acidity function in amorphous solids using inversion of sucrose as a model reaction.

    abstract::The goal was to evaluate the effects of acidity, expressed as the Hammett acidity function, on chemical reactivity in freeze-dried materials (lyophiles). Dextran-sucrose-citrate and polyvinyl pyrrolidone (PVP)-sucrose-citrate aqueous solutions, adjusted to pH values of 2.6, 2.8, and 3.0 were freeze dried, and characte...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21081

    authors: Chatterjee K,Shalaev EY,Suryanarayanan R,Govindarajan R

    更新日期:2008-01-01 00:00:00

  • Coloaded Nanoparticles of Paclitaxel and Piperlongumine for Enhancing Synergistic Antitumor Activities and Reducing Toxicity.

    abstract::The purpose of this study was to develop a nanocarrier system for codelivery of paclitaxel (PTX) and piperlongumine (PL) and investigate the therapeutic potential of improving efficacy and reducing toxicity. PTX and PL were formulated into poly lactic-co-glycolic acid and D-α-tocopheryl polyethylene glycol succinate v...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.05.027

    authors: Liu Q,Zhao D,Zhu X,Chen H,Yang Y,Xu J,Zhang Q,Fan A,Li N,Guo C,Kong Y,Lu Y,Chen X

    更新日期:2017-10-01 00:00:00

  • Novel method of derivatization of an amidinourea (lidamidine) for GLC analysis.

    abstract::A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710327

    authors: Won CM,Zalipsky JJ,Patel DM,Grim WM

    更新日期:1982-03-01 00:00:00

  • Cholesterol-mediated activation of P-glycoprotein: distinct effects on basal and drug-induced ATPase activities.

    abstract::Cholesterol promotes basal and verapamil-induced ATPase activity of P-glycoprotein (P-gp). We investigated whether these effects are related to each other and to the impact of the sterol on bilayer fluidity and verapamil membrane affinity. P-gp was reconstituted in egg-phosphatidylcholine (PhC) liposomes with or witho...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21558

    authors: Belli S,Elsener PM,Wunderli-Allenspach H,Krämer SD

    更新日期:2009-05-01 00:00:00

  • Bioavailability of seocalcitol I: Relating solubility in biorelevant media with oral bioavailability in rats--effect of medium and long chain triglycerides.

    abstract::Simulated intestinal media (SIM) containing bile salt (BS) and phospholipids (PL) with and without medium chain lipolytic products (MC-LP) or long chain lipolytic products (LC-LP) were developed to study the solubility of seocalcitol. Both MC-LP and LC-LP were studied in order to investigate the influence of fatty aci...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20403

    authors: Grove M,Pedersen GP,Nielsen JL,Müllertz A

    更新日期:2005-08-01 00:00:00

  • Influence of excipients, drugs, and osmotic agent in the inner core on the time-controlled disintegration of compression-coated ethylcellulose tablets.

    abstract::The effect of excipient, drug, and osmotic agent loaded in the inner core tablet on the time-controlled disintegration of compression-coated tablet prepared by direct compression with micronized ethylcellulose was investigated. The excipients [spray-dried lactose, hydroxypropyl methyl cellulose, sodium starch glycolat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10197

    authors: Lin SY,Lin KH,Li MJ

    更新日期:2002-09-01 00:00:00

  • Influence of solid phase and formulation processing on stability of Abbott-232 tablet formulations.

    abstract::Abbott-232 is a chemically stable, highly water soluble non-hygroscopic compound selected for development as a potent uroselective alpha(1A) agonist. An anhydrate, a monohydrate, and an amorphous phase were isolated. The anhydrate was chosen for formulation development based on solid-state characterization. Excipients...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20679

    authors: Wardrop J,Law D,Qiu Y,Engh K,Faitsch L,Ling C

    更新日期:2006-11-01 00:00:00

  • Evaluation of 2-azabicyclo[2.2..2]octane analogs of 4-anilidopiperidine analgesics.

    abstract::Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690934

    authors: Borne RF,Law SJ,Kapeghian JC,Masten LW

    更新日期:1980-09-01 00:00:00

  • Improved delivery through biological membranes XD: Percutaneous absorption and metabolism of methylsulfinylmethyl 2-acetoxybenzoate and related aspirin prodrugs.

    abstract::Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700710

    authors: Loftsson T,Bodor N

    更新日期:1981-07-01 00:00:00