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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/28785860/improved-oral-bioavailability-therapeutic-efficacy-and-reduced-toxicity-of-tamoxifen-loaded-liquid-crystalline-nanoparticles
#1
Sanyog Jain, B Heeralal, Rajan Swami, Nitin K Swarnakar, Varun Kushwah
Present investigation deals with formulation and evaluation of tamoxifen (TMX)-loaded liquid crystalline nanoparticles (TMX-LCNPs) for improving oral bioavailability and safety of the existing treatment. Hexagonal Glyceryl monooleate-based TMX-LCNPs (GLCNPs) and Phytantriol-based TMX-LCNPs (PLCNPs) were prepared by dilution-through-hydrotrope method for oral administration. Oleic acid was incorporated in the lipid matrix to enhance the drug loading in the LCNPs. Optimized LCNPs displayed small particle size with a narrow distribution, sustained drug release and high gastrointestinal stability...
August 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28785859/application-of-optical-coherence-tomography-freeze-drying-microscopy-for-designing-lyophilization-process-and-its-impact-on-process-efficiency-and-product-quality
#2
Maxwell Korang-Yeboah, Charudharshini Srinivasan, Akhtar Siddiqui, David Awotwe-Otoo, Celia N Cruz, Ashraf Muhammad
Optical coherence tomography freeze-drying microscopy (OCT-FDM) is a novel technique that allows the three-dimensional imaging of a drug product during the entire lyophilization process. OCT-FDM consists of a single-vial freeze dryer (SVFD) affixed with an optical coherence tomography (OCT) imaging system. Unlike the conventional techniques, such as modulated differential scanning calorimetry (mDSC) and light transmission freeze-drying microscopy, used for predicting the product collapse temperature (Tc), the OCT-FDM approach seeks to mimic the actual product and process conditions during the lyophilization process...
August 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28770529/effect-of-surfactants-on-mechanical-thermal-and-photostability-of-a-monoclonal-antibody
#3
Meera Agarkhed, Courtney O'Dell, Ming-Ching Hsieh, Jingming Zhang, Joel Goldstein, Arvind Srivastava
The purpose of this work was to evaluate the effect of commonly used surfactants (at 0.01% w/v concentration) on mechanical, thermal, and photostability of a monoclonal antibody (MAb1) of IgG1 sub-class and to evaluate the minimum concentration of surfactant (Polysorbate 80) required in protecting MAb1 from mechanical stress. Surfactants evaluated were non-ionic surfactants, Polysorbate 80, Polysorbate 20, Pluronic F-68 (polyoxyethylene-polyoxypropylene block polymer), Brij 35 (polyoxyethylene lauryl ether), Triton X-100, and an anionic surfactant, Caprylic acid (1-Heptanecarboxylic acid)...
August 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28770528/quiescent-and-agitated-redispersion-as-a-tool-for-evaluating-dispersant-effectiveness-in-dissolution-enhancement-of-drug-laden-nanocomposites
#4
A Bhakay, R N Davé, E Bilgili
Nanocomposite microparticles (NCMPs) have been used in various solid dosage forms with the goal of enhancing the dissolution rate and bioavailability of poorly water-soluble drugs. Nanoparticle recovery from NCMPs, i.e., redispersion, is the preliminary step in drug dissolution. This study aims at exploring aqueous redispersion of NCMPs with various dispersants under quiescent vs. agitated conditions as potential dispersant screening tool in the development of fast-dissolving NCMP formulations. NCMPs were prepared by coating wet-milled suspensions of a poorly water-soluble drug, griseofulvin (GF), formulated with the dispersants hydroxypropyl cellulose (HPC), sodium dodecyl sulfate (SDS), as-received/wet co-milled croscarmellose sodium (CCS), and mannitol, onto Pharmatose® carrier particles in a fluidized bed dryer...
August 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28762212/experimental-studies-and-modeling-of-the-drying-kinetics-of-multicomponent-polymer-films
#5
Sitaram P Velaga, Dariush Nikjoo, Parameswara R Vuddanda
The process of drying thin polymer films is an important operation that influences the film structure and solid state, and the stability of the product. The purpose of this work was to study and model the drying kinetics of multicomponent films based on two polymers: hydroxypropyl methylcellulose (HPMC, amorphous) and polyvinyl alcohol (PVA, semicrystalline). The isothermal drying kinetics of the films at different temperatures (40, 60, and 80°C) were studied using thermo-gravimetric analysis (TGA) and convection oven methods...
July 31, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28755053/commentary-why-pharmaceutical-scientists-in-early-drug-discovery-are-critical-for-influencing-the-design-and-selection-of-optimal-drug-candidates
#6
Margaret S Landis, Shobha Bhattachar, Mehran Yazdanian, John Morrison
This commentary reflects the collective view of pharmaceutical scientists from four different organizations with extensive experience in the field of drug discovery support. Herein, engaging discussion is presented on the current and future approaches for the selection of the most optimal and developable drug candidates. Over the past two decades, developability assessment programs have been implemented with the intention of improving physicochemical and metabolic properties. However, the complexity of both new drug targets and non-traditional drug candidates provides continuing challenges for developing formulations for optimal drug delivery...
July 28, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28755052/usp-apparatus-4-a-valuable-in-vitro-tool-to-enable-formulation-development-of-long-acting-parenteral-lap-nanosuspension-formulations-of-poorly-water-soluble-compounds
#7
William P Forrest, Kevin G Reuter, Vivek Shah, Irina Kazakevich, Michael Heslinga, Siddhi Dudhat, Sanjaykumar Patel, Claudia Neri, Yun Mao
Long-acting or extended release parenteral dosage forms have attracted extensive attention due to their ability to maintain therapeutic drug concentrations over long periods of time and reduce administration frequency, thus improving patient compliance. It is essential to have an in vitro release (IVR) testing method that can be used to assure product quality during routine production as well as predict and understand the in vivo performance of a formulation. The purpose of this work was to develop a discriminatory in vitro release method to guide formulation and process development of long-acting parenteral (LAP) nanosuspension formulations composed of poorly water-soluble drugs (BCS class II)...
July 28, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28752471/calcium-phosphate-particles-as-pulmonary-delivery-system-for-interferon-%C3%AE-in-mice
#8
Tülin Morçöl, Jessica M Weidner, Anand Mehta, Stephen J D Bell, Timothy Block
Systemically administered interferons are rapidly cleared from the circulation thus requiring frequent dosing to maintain the therapeutic levels of circulating interferon. This is particularly problematic for their use in the treatment of chronic diseases. The purpose of this study was to evaluate the potential of proprietary calcium phosphate (CaP) particles to deliver biologically active interferon alpha (IFNα) via the lungs into systemic circulation. Recombinant human IFNα-2a was formulated with proprietary CaP particles...
July 27, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28748368/development-and-evaluation-of-ph-responsive-cyclodextrin-based-in-situ-gel-of-paliperidone-for-intranasal-delivery
#9
Atul P Sherje, Vaishali Londhe
Paliperidone (PLPD) is approved for treatment and management of schizophrenia. The current study demonstrates the potential of in situ gel of PLPD for nasal delivery. The permeation of drug through sheep nasal mucosa was analyzed since the nose-to-brain pathway has been indicated for delivering drugs to the brain. The carbopol 934 (CP)- and hydroxypropyl methyl cellulose K4M (HPMC)-based in situ gels containing 0.2% CP and 0.4% w/v HPMC were optimized using experimental design software. The use of hydroxypropyl-β-cyclodextrin (HP-β-CD) in nasal permeation of drug was investigated...
July 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28741140/melt-extrusion-for-a-high-melting-point-compound-with-improved-solubility-and-sustained-release
#10
Jiannan Lu, Sakae Obara, Fei Liu, Wanyi Fu, Wen Zhang, Shingo Kikuchi
The objective of the current study was to develop an amorphous solid dispersion for a high melting point compound, griseofulvin (GRF), with an enhanced solubility and a controlled release pattern utilizing hot melt extrusion (HME) technology. Hypromellose acetate succinate (HPMCAS, Shin-Etsu AQOAT®, medium particle size) was explored as the polymeric carrier, while hypromellose (HPMC, Metolose® SR) was chosen as the release rate control agent. GRF presented an HPMCAS grade-dependent solubility: AS-HMP > AS-MMP > AS-LMP...
July 24, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28741139/characterization-of-a-liquid-crystal-system-for-sustained-release-of-a-peptide-bms-686117
#11
Yan Xu, Vivian Li, Jinjiang Li, Duohai Pan, Gerd Langenbucher, Neil Mathias
Liquid crystal lipid-based formulations are an effective approach to prolong pharmacokinetics and reduce burst release of a drug on subcutaneous delivery. The objective of this paper was to investigate the influence of phase structures of a lipid-based liquid crystal delivery system and its associated mechanical properties on the release profile of a peptide. It was hypothesized that release of drug molecules are closely related to the mechanical properties that are controlled by phase structures. Experimentally, the relationship between phase structures of lipid liquid crystal system-soy phosphatidyl choline (SPC) and glycerol dioleate (GDO) in water were characterized by polarized light microscopy and small angle X-ray diffraction...
July 24, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28733828/thermosensitive-in-situ-gel-based-on-solid-dispersion-for-rectal-delivery-of-ibuprofen
#12
Yangdan Liu, Xin Wang, Youping Liu, Xin Di
The objective of this study was to develop a thermosensitive in situ gel based on solid dispersions (SDs) for rectal delivery of ibuprofen (IBU). Thermosensitive (poloxamer 407) and mucoadhesive (hydroxypropylmethyl cellulose E5 and sodium alginate) polymers were used to prepare the in situ gel and the sol-gel transition temperature (T sol-gel) and gel strength were optimized. The in vitro release performance and in vivo pharmacokinetic properties of the in situ gel after their rectal administration to rabbits were investigated...
July 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28721630/in-situ-salification-in-polar-solvents-a-paradigm-for-enabling-drug-delivery-of-weakly-ionic-drugs-as-amorphous-solid-dispersion
#13
Rashmi Nair, Ioorika Lamare, Nirbhay Kumar Tiwari, Punna Rao Ravi, Raviraj Pillai
Solubility challenge for a poorly water-soluble drug gets further intensified when it is weakly ionic because the most common solubility enhancement technique, salt formation, becomes less feasible. Salt screening for such drugs often concludes with either a difficult to crystalize salt or an unstable salt, leading the scientists to explore other solubility enhancement technique like amorphous solid dispersions which is comparatively costlier, time-consuming and may require use of hazardous organic solvents...
July 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28717975/development-of-a-novel-polymeric-nanocomposite-complex-for-drugs-with-low-bioavailability
#14
Mduduzi N Sithole, Yahya E Choonara, Lisa C du Toit, Pradeep Kumar, Thashree Marimuthu, Pierre P D Kondiah, Viness Pillay
Semi-synthetic biopolymer complex (SSBC) nanoparticles were investigated as a potential oral drug delivery system to enhance the bioavailability of a poorly water-soluble model drug acyclovir (ACV). The SSBCs were prepared from cross-linking of hydroxyl groups on hyaluronic acid (HA) with poly(acrylic acid) (PAA) resulting in ether linkages. Thereafter, conjugation of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) onto HA-PAA was accomplished using a 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC)/N-hydroxysuccinimide (NHS)-promoted coupling reaction...
July 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28717974/improvement-of-oral-bioavailability-of-lopinavir-without-co-administration-of-ritonavir-using-microspheres-of-thiolated-xyloglucan
#15
Ashwini R Madgulkar, Mangesh R Bhalekar, Ashwini A Kadam
Lopinavir is a BCS Class IV drug exhibiting poor bioavailability due to P-gp efflux and limited permeation. The aim of this research was to formulate and characterize microspheres of lopinavir using thiolated xyloglucan (TH-MPs) as carrier to improve its oral bioavailability without co-administration of ritonavir. Thiomeric microspheres were prepared by ionotropic gelation between alginic acid and calcium ions. Interaction studies were performed using Fourier transform infrared spectroscopy (FT-IR). The thiomeric microspheres were characterized for its entrapment efficiency, T80, surface morphology, and mucoadhesion employing in vitro wash off test...
July 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28717973/design-and-development-of-repaglinide-microemulsion-gel-for-transdermal-delivery
#16
Ujwala A Shinde, Sheela H Modani, Kavita H Singh
Microemulsion formulation of repaglinide, a BCS class II hypoglycemic agent with limited oral bioavailability, was developed considering its solubility in various oils, surfactants, and cosurfactants. The pseudo-ternary phase diagrams for microemulsion regions were constructed by water titration method at K m 1:1 and characterized for optical birefringence, percentage transmittance, pH, refractive index, globule size, zeta potential, viscosity, drug content, and thermodynamic stability. To enhance the drug permeation and residence time, the optimized microemulsions having mean globule size of 36...
July 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28702817/tamibarotene-loaded-plga-microspheres-for-intratumoral-injection-administration-preparation-and-evaluation
#17
Liu Tian, Jinhua Gao, Zhenlei Yang, Zhihua Zhang, Guihua Huang
Tamibarotene (Am80) has good curative effect on advanced hepatocellular carcinoma (HCC). To improve the therapeutic efficacy furtherly, we prepared tamibarotene-loaded PLGA microspheres (Am80-PLGA-MS) for intratumoral injection. Firstly, Am80-PLGA-MS were prepared by emulsion-solvent evaporation method. Subsequently, microspheres were characterized by particle size analysis, drug loading (DL), and entrapment efficiency (EE). Finally, the drug release characteristics in vitro, pharmacokinetic, and pharmacodynamics were studied separately...
July 12, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28702816/enhancing-the-solubility-of-fenofibrate-by-nanocrystal-formation-and-encapsulation
#18
Raj Kumar, Prem Felix Siril
Development of techniques to enhance bioavailability of drugs having poor water solubility is a big challenge for pharmaceutical industry. Solubility can be enhanced by particle size reduction and encapsulation using hydrophilic polymers. Fenofibrate (FF) is a drug for regulating lipids. Multi-fold enhancement in solubility of FF has been achieved by nanocrystal formation in the present study. Nanoparticles were prepared by an evaporation-assisted solvent-antisolvent interaction (EASAI) approach. Water-soluble polymers, viz...
July 12, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28698930/proliposome-powders-for-the-generation-of-liposomes-the-influence-of-carbohydrate-carrier-and-separation-conditions-on-crystallinity-and-entrapment-of-a-model-antiasthma-steroid
#19
Iftikhar Khan, Sakib Yousaf, Sneha Subramanian, Mohamed Albed Alhnan, Waqar Ahmed, Abdelbary Elhissi
Formulation effects on the entrapment of beclometasone dipropionate (BDP) in liposomes generated by hydration of proliposomes were studied, using the high-density dispersion medium deuterium oxide in comparison to deionized water (DW). Proliposomes incorporating BDP (2 mol% of the lipid phase consisting of soya phosphatidylcholine (SPC) and cholesterol; 1:1) were manufactured, using lactose monohydrate (LMH), sorbitol or D-mannitol as carbohydrate carriers (1:5 w/w lipid to carrier). Following hydration of proliposomes, separation of BDP-entrapped liposomes from the unentrapped (free) BDP at an optimized centrifugation duration of 90 min and a centrifugation force of 15,500g were identified...
July 11, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28695328/study-of-the-emitted-dose-after-two-separate-inhalations-at-different-inhalation-flow-rates-and-volumes-and-an-assessment-of-aerodynamic-characteristics-of-indacaterol-onbrez-breezhaler-%C3%A2-150-and-300%C3%A2-%C3%AE-g
#20
Mohamad Abadelah, Henry Chrystyn, Golshan Bagherisadeghi, Gaballa Abdalla, Hassan Larhrib
Onbrez Breezhaler® is a low-resistance capsule-based device that was developed to deliver indacaterol maleate. The study was designed to investigate the effects of both maximum flow rate (MIF) and inhalation volume (Vin) on the dose emission of indacaterol 150 and 300 μg dose strengths after one and two inhalations using dose unit sampling apparatus (DUSA) as well as to study the aerodynamic characteristics of indacaterol Breezhaler® using the Andersen cascade impactor (ACI) at a different set of MIF and Vin...
July 10, 2017: AAPS PharmSciTech
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