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    2411 results match your criteria AAPS PharmSciTech[Journal]

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    Magnetic Nanoparticles for the Delivery of Dapagliflozin to Hypoxic Tumors: Physicochemical Characterization and Cell Studies.
    AAPS PharmSciTech 2017 Sep 18. Epub 2017 Sep 18.
    Department of Pharmacy, Medical School, University of Patras, 26504, Patras, Greece.
    In solid tumors, hypoxia (lack of oxygen) is developed, which leads to the development of resistance of tumor cells to chemotherapy and radiotherapy through various mechanisms. Nevertheless, hypoxic cells are particularly vulnerable when glycolysis is inhibited. For this reason, in this study, the development of magnetically targetable nanocarriers of the sodium-glucose transporter protein (SGLT2) inhibitor dapagliflozin (DAPA) was developed for the selective delivery of DAPA in tumors. Read More

    Effects of the Preparation Process on the Properties of Amorphous Solid Dispersions.
    AAPS PharmSciTech 2017 Sep 18. Epub 2017 Sep 18.
    Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, Mail Stop A1920, Austin, Texas, USA.
    The use of amorphous solid dispersions to improve the bioavailability of active ingredients from the BCS II and IV classifications continues to gain interest in the pharmaceutical industry. Over the last decade, methods for generating amorphous solid dispersions have been well established in commercially available products and in the literature. However, the amorphous solid dispersions manufactured by different technologies differ in many aspects, primarily chemical stability, physical stability, and performance, both in vitro and in vivo. Read More

    Preparation, Characterization and In Vitro / In Vivo Evaluation of Oral Time-Controlled Release Etodolac Pellets.
    AAPS PharmSciTech 2017 Sep 15. Epub 2017 Sep 15.
    Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning Province, 110016, China.
    The objective of this study was to prepare time-controlled release etodolac pellets to facilitate drug administration according to the body's biological rhythm, optimize the drug's desired effects, and minimize adverse effects. The preparation consisted of three laminal layers from center to outside: the core, the swelling layer, and the insoluble polymer membrane. Factors influenced the core and the coating films were investigated in this study. Read More

    Development of a Mini-Freeze Dryer for Material-Sparing Laboratory Processing with Representative Product Temperature History.
    AAPS PharmSciTech 2017 Sep 13. Epub 2017 Sep 13.
    Department of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut, 06269, USA.
    The goal of the work described in this publication was to evaluate a new, small, material-sparing freeze dryer, denoted as the "mini-freeze dryer or mini-FD", capable of reproducing the product temperature history of larger freeze dryers, thereby facilitating scale-up. The mini-FD wall temperatures can be controlled to mimic loading procedures and dryer process characteristics of larger dryers. The mini-FD is equipped with a tunable diode laser absorption spectroscopy (TDLAS) water vapor mass flow monitor and with other advanced process analytical technology (PAT) sensors. Read More

    Photostability Issues in Pharmaceutical Dosage Forms and Photostabilization.
    AAPS PharmSciTech 2017 Sep 13. Epub 2017 Sep 13.
    Department of Pharmaceutics and Drug Delivery, The University of Mississippi, University, MS, 38677, USA.
    Photodegradation is one of the major pathways of the degradation of drugs. Some therapeutic agents and excipients are highly sensitive to light and undergo significant degradation, challenging the quality and the stability of the final product. The adequate knowledge of photodegradation mechanisms and kinetics of photosensitive therapeutic entities or excipients is a pivotal aspect in the product development phase. Read More

    Stability of Organoleptic Agents in Pharmaceuticals and Cosmetics.
    AAPS PharmSciTech 2017 Sep 12. Epub 2017 Sep 12.
    Department of Pharmaceutics and Drug Delivery, University of Mississippi, University, MS, USA.
    Organoleptic agents constitute an important niche in the field of pharmaceutical excipients. These agents encompass a range of additives responsible for coloring, flavoring, sweetening, and texturing formulations. All these agents have come to play a significant role in pharmaceuticals and cosmetics due to their ability to increase patient compliance by elevating a formulation's elegance and esthetics. Read More

    Excipient Stability in Oral Solid Dosage Forms: A Review.
    AAPS PharmSciTech 2017 Sep 11. Epub 2017 Sep 11.
    Department of Pharmaceutics and Drug Delivery, The University of Mississippi, University, MS, 38677, United States.
    The choice of excipients constitutes a major part of preformulation and formulation studies during the preparation of pharmaceutical dosage forms. The physical, mechanical, and chemical properties of excipients affect various formulation parameters, such as disintegration, dissolution, and shelf life, and significantly influence the final product. Therefore, several studies have been performed to evaluate the effect of drug-excipient interactions on the overall formulation. Read More

    Solid-State Stability Issues of Drugs in Transdermal Patch Formulations.
    AAPS PharmSciTech 2017 Sep 11. Epub 2017 Sep 11.
    Department of Pharmaceutics and Drug Delivery, The University of Mississippi, 113 Faser Hall, University, Mississippi, 38677, USA.
    The transdermal patch formulation has many advantages, including noninvasiveness, an ability to bypass the first-pass metabolism, low dosage requirements, and prolonged drug delivery. However, the instability of solid-state drugs is one of the most critical problems observed in transdermal patch products. Therefore, a well-characterized approach for counteracting stability problems in solid-state drugs is crucial for improving the performance of transdermal patch products. Read More

    Optimization of Curcuma Oil/Quinine-Loaded Nanocapsules for Malaria Treatment.
    AAPS PharmSciTech 2017 Sep 5. Epub 2017 Sep 5.
    Curso de Farmácia, Universidade Federal do Pampa, UNIPAMPA, Uruguaiana, RS, 97500-970, Brazil.
    Quinine, a treatment used in chloroquine-resistant falciparum malaria, was loaded into poly(ɛ-caprolactone) or Eudragit(®) RS100 nanocapsules using Curcuma oil as the oil-based core. Until now, the effect of cationic nanocapsules on malaria has not been reported. A 2(4) factorial design was adopted using, as independent variables, the concentration of Curcuma oil, presence of quinine, type of polymer, and aqueous surfactant. Read More

    Albumin-Conjugated Lipid-Based Multilayered Nanoemulsion Improves Drug Specificity and Anti-Inflammatory Potential at the Spinal Cord Injury gSite after Intravenous Administration.
    AAPS PharmSciTech 2017 Sep 5. Epub 2017 Sep 5.
    Department of Orthopedics, Huai'an First People's Hospital, Nanjing Medical University, 6 Beijing Road West, Huai'an, Jiangsu, 223300, China.
    Albumin-conjugated multilayered nanoemulsion (albumin-MNE) of methyl prednisolone (MP) was developed to ensure the specificity of the drug at the spinal cord injury (SCI) site. MNE was prepared by emulsification followed by ionic deposition of oppositely charged polymer followed by albumin conjugation using N-hydroxysuccinimide. Prepared nanoemulsion was characterized for particle size, polydispersity index (PDI), zeta potential (Zp), pH, viscosity, and entrapment efficiency. Read More

    Laboratory Study Comparing Pharmacopeial Testing of Nebulizers with Evaluation Based on Nephele Mixing Inlet Methodology.
    AAPS PharmSciTech 2017 Sep 5. Epub 2017 Sep 5.
    S5 Consulting Blentarp, SE-27562, Blentarp, Sweden.
    Determination of fine droplet dose with preparations for nebulization, currently deemed to be the metric most indicative of lung deposition and thus in vivo responses, involves combining two procedures following practice as described in the United States Pharmacopeia and the European Pharmacopeia. Delivered dose (DD) is established by simulating tidal breathing at the nebulizer, collecting the medication on a filter downstream of the nebulizer mouthpiece/facemask. Fine droplet fraction (FDFRead More

    Appraisal of Transdermal Water-in-Oil Nanoemulgel of Selegiline HCl for the Effective Management of Parkinson's Disease: Pharmacodynamic, Pharmacokinetic, and Biochemical Investigations.
    AAPS PharmSciTech 2017 Sep 5. Epub 2017 Sep 5.
    Nanoformulation Laboratory, Department of Pharmaceutics, School of Pharmaceutical Education and Research (erstwhile Faculty of Pharmacy), Jamia Hamdard, New Delhi, 110062, India.
    In the present study, the potential of transdermal nanoemulsion gel of selegiline hydrochloride for the treatment of Parkinson's disease was investigated. Water-in-oil nanoemulsions were developed by comparing low- and high-energy methods and were subjected to thermodynamic stability tests, in vitro permeation, and characterization studies. In vitro studies indicated that components of nanoemulsion acted as permeation enhancers with highest flux of 3. Read More

    Formulation Screening and Freeze-Drying Process Optimization of Ginkgolide B Lyophilized Powder for Injection.
    AAPS PharmSciTech 2017 Aug 28. Epub 2017 Aug 28.
    School of Engineering, China Pharmaceutical University, Nanjing, China.
    The purpose of this study was to prepare ginkgolide B (GB) lyophilized powder for injection with excellent appearance and stable quality through a formulation screening and by optimizing the freeze-drying process. Cremophor EL as a solubilizer, PEG 400 as a latent solvent, and mannitol as an excipient were mixed to increase the solubility of GB in water to more than 18 times (about from 2.5 × 10(-4) mol/L (0. Read More

    Co-Spray Dried Mannitol/Poly(amidoamine)-Doxorubicin Dry-Powder Inhaler Formulations for Lung Adenocarcinoma: Morphology, In Vitro Evaluation, and Aerodynamic Performance.
    AAPS PharmSciTech 2017 Aug 23. Epub 2017 Aug 23.
    Department of Radiology, School of Medicine, Stanford University, Palo Alto, California, 94304, USA.
    nhaled chemotherapeutics have emerged as a promising regimen to combat lung cancer as they maximize local drug concentration while significantly reduce systemic exposure. However, the poor lung/systemic safety profiles and lack of clinically efficient formulations restrict the applicability of inhaled chemotherapeutics. This work developed a dry-powder inhaler (DPI) formulation that dispersed a pH-responsive poly(amidoamine) dendrimer-doxorubicin conjugate (G4-12DOX) into mannitol microparticles. Read More

    Cationic Niosomes for Enhanced Skin Immunization of Plasmid DNA-Encoding Ovalbumin via Hollow Microneedles.
    AAPS PharmSciTech 2017 Aug 21. Epub 2017 Aug 21.
    Faculty of Pharmacy, Pharmaceutical Development of Green Innovations Group (PDGIG), Silpakorn University, Nakhon Pathom, 73000, Thailand.
    The purpose of the present study was to evaluate the use of cationic niosomes composed of Span20:cholesterol:cationic lipid (N (1),N (1)-dimyristeroyloxyethyl-spermine) at the molar ratio of 2.5:2.5:0. Read More

    Dissolution Test of Tacrolimus Capsule: Effects of Filtration and Glass Adsorption.
    AAPS PharmSciTech 2017 Aug 21. Epub 2017 Aug 21.
    Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, 10903 New Hampshire Ave, Silver Spring, Maryland, USA.
    Tacrolimus is a potent, narrow therapeutic index, immunosuppressive drug used to avoid organ rejection in patients that have undergone organ transplantation. Dissolution tests are widely used to evaluate drug product quality and performance. Analysis of tacrolimus during dissolution testing is sensitive to several factors, such as sample solution storage time and container material. Read More

    Anti-inflammatory Effect from a Hydrogel Containing Nanoemulsified Copaiba oil (Copaifera multijuga Hayne).
    AAPS PharmSciTech 2017 Aug 21. Epub 2017 Aug 21.
    Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga 2752, Laboratório 606, Porto Alegre, RS, 90610-000, Brazil.
    Copaiba oil is used as a popular medicine in the Amazonian forest region, especially due to its anti-inflammatory properties. In this paper, we describe the formulation of hydrogel containing copaiba oil nanoemulsions (with positive and negative charges), its skin permeation, and its anti-inflammatory activity in two in vivo models: mouse ear edema and rat paw edema. Three hydrogels were tested (Carbopol(®), hydroxyethylcellulose and chitosan), but only Carbopol(®) and hydroxyethylcellulose hydrogels presented good stability and did not interfere with the nanoemulsions droplet size and polydispersity index. Read More

    Formulation and In Vitro Release Kinetics of Mucoadhesive Blend Gels Containing Matrine for Buccal Administration.
    AAPS PharmSciTech 2017 Aug 21. Epub 2017 Aug 21.
    Department of Pharmacy, Hangzhou Children's Hospital, No.195, Wenhui Road, Xiacheng District, Hangzhou City, Zhejiang Province, 310014, China.
    Enterovirus 71 (EV71) is a pathogenic factor of severe hand, foot, and mouth disease (HFMD). No vaccine or specific treatment is currently available for EV71 infection. Hence, we developed a buccal mucoadhesive gel containing matrine to protect against HFMD. Read More

    Improved Oral Bioavailability, Therapeutic Efficacy, and Reduced Toxicity of Tamoxifen-Loaded Liquid Crystalline Nanoparticles.
    AAPS PharmSciTech 2017 Aug 7. Epub 2017 Aug 7.
    Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar (Mohali), Punjab, 160062, India.
    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. Read More

    Application of Optical Coherence Tomography Freeze-Drying Microscopy for Designing Lyophilization Process and Its Impact on Process Efficiency and Product Quality.
    AAPS PharmSciTech 2017 Aug 7. Epub 2017 Aug 7.
    Division of Product Quality Research, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, Food and Drug Administration, White Oak, LS Building 64, 10903 New Hampshire Ave, Silver Spring, Maryland, 20993-002, USA.
    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. Read More

    Effect of Surfactants on Mechanical, Thermal, and Photostability of a Monoclonal Antibody.
    AAPS PharmSciTech 2017 Aug 2. Epub 2017 Aug 2.
    Formulation Development, Eli Lilly and Company, 59-61 ImClone Drive, Branchburg, NJ, 08876, USA.
    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). Read More

    Quiescent and Agitated Redispersion as a Tool for Evaluating Dispersant Effectiveness in Dissolution Enhancement of Drug-Laden Nanocomposites.
    AAPS PharmSciTech 2017 Aug 2. Epub 2017 Aug 2.
    Otto H. York Department of Chemical, Biological, and Pharmaceutical Engineering, New Jersey Institute of Technology, 161 Warren St. 150 Tiernan Hall, Newark, New Jersey, 07102, USA.
    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. Read More

    Experimental Studies and Modeling of the Drying Kinetics of Multicomponent Polymer Films.
    AAPS PharmSciTech 2017 Jul 31. Epub 2017 Jul 31.
    Pharmaceutical and biomaterials research, Department of Health Sciences, Luleå University of Technology, SE-97187, Luleå, Sweden.
    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. Read More

    Commentary: Why Pharmaceutical Scientists in Early Drug Discovery Are Critical for Influencing the Design and Selection of Optimal Drug Candidates.
    AAPS PharmSciTech 2017 Jul 28. Epub 2017 Jul 28.
    Discovery Pharmaceutics, Bristol-Myers Squibb, Wallingford, Connecticut, 06492, USA.
    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. Read More

    USP Apparatus 4: a Valuable In Vitro Tool to Enable Formulation Development of Long-Acting Parenteral (LAP) Nanosuspension Formulations of Poorly Water-Soluble Compounds.
    AAPS PharmSciTech 2017 Jul 28. Epub 2017 Jul 28.
    Analytical Sciences, MRL, Merck & Co., Inc., Rahway, New Jersey, 07065, USA.
    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). Read More

    Calcium Phosphate Particles as Pulmonary Delivery System for Interferon-α in Mice.
    AAPS PharmSciTech 2017 Jul 27. Epub 2017 Jul 27.
    Baruch S. Blumberg Institute and Hepatitis B Foundation, Doylestown, Pennsylvania, USA.
    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. Read More

    Development and Evaluation of pH-Responsive Cyclodextrin-Based in situ Gel of Paliperidone for Intranasal Delivery.
    AAPS PharmSciTech 2017 Jul 26. Epub 2017 Jul 26.
    Department of Pharmaceutics, SPP School of Pharmacy & Technology Management, SVKM's NMIMS, Vile Parle (W), Mumbai, 400056, India.
    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. Read More

    Palm Olein Emulsion: a Novel Vehicle for Topical Drug Delivery of Betamethasone 17-Valerate.
    AAPS PharmSciTech 2017 Jul 25. Epub 2017 Jul 25.
    Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia, 25200, Kuantan, Malaysia.
    This study aims to investigate the use of palm olein as the oil phase for betamethasone 17-valerate (BV) emulsions. The physicochemical properties of the formulations were characterized. In vitro drug release study was performed with the Hanson Vertical Diffusion Cell System; the samples were quantified with HPLC and the results were compared with commercial products. Read More

    Melt Extrusion for a High Melting Point Compound with Improved Solubility and Sustained Release.
    AAPS PharmSciTech 2017 Jul 24. Epub 2017 Jul 24.
    Cellulose Technical Support Center, Shin-Etsu Chemical Co. Ltd., Yokohama, Kanagawa, 240-0005, Japan.
    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. Read More

    Characterization of a Liquid Crystal System for Sustained Release of a Peptide BMS-686117.
    AAPS PharmSciTech 2017 Jul 24. Epub 2017 Jul 24.
    Drug Product Science and Technology, Bristol-Myers Squibb, New Brunswick, New Jersey, 08903, USA.
    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. Read More

    Thermosensitive In Situ Gel Based on Solid Dispersion for Rectal Delivery of Ibuprofen.
    AAPS PharmSciTech 2017 Jul 21. Epub 2017 Jul 21.
    Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, People's Republic of China.
    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. Read More

    In Situ Salification in Polar Solvents: a Paradigm for Enabling Drug Delivery of Weakly Ionic Drugs as Amorphous Solid Dispersion.
    AAPS PharmSciTech 2017 Jul 18. Epub 2017 Jul 18.
    Innovations & Development, Abbott Healthcare Pvt. Ltd., Hiranandani Business Park, Saki Vihar Road, Chandivali, Andheri West, Mumbai, 400072, India.
    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. Present study evaluated in situ salification in polar protic solvents for dissolving poorly water-soluble drug Itraconazole which is weakly ionic and not very amenable to formation of stable inorganic salts. Read More

    Development of a Novel Polymeric Nanocomposite Complex for Drugs with Low Bioavailability.
    AAPS PharmSciTech 2017 Jul 17. Epub 2017 Jul 17.
    Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown, Johannesburg, 2193, South Africa.
    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. Read More

    Improvement of Oral Bioavailability of Lopinavir Without Co-administration of Ritonavir Using Microspheres of Thiolated Xyloglucan.
    AAPS PharmSciTech 2017 Jul 17. Epub 2017 Jul 17.
    AISSMS College of Pharmacy, Pune, Maharashtra, 411001, India.
    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. Read More

    Design and Development of Repaglinide Microemulsion Gel for Transdermal Delivery.
    AAPS PharmSciTech 2017 Jul 17. Epub 2017 Jul 17.
    SPP School of Pharmacy and Technology Management, NMIMS University, Mumbai, 400056, India.
    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. Read More

    Tamibarotene-Loaded PLGA Microspheres for Intratumoral Injection Administration: Preparation and Evaluation.
    AAPS PharmSciTech 2017 Jul 12. Epub 2017 Jul 12.
    The School of Pharmaceutical Science, Shandong University, 44 Wenhua Xi Road, Jinan, Shandong Province, People's Republic of China.
    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. Read More

    Enhancing the Solubility of Fenofibrate by Nanocrystal Formation and Encapsulation.
    AAPS PharmSciTech 2017 Jul 12. Epub 2017 Jul 12.
    School of Basic Sciences and Advanced Material Research Centre, Indian Institute of Technology Mandi, Mandi, Himachal Pradesh, 175005, India.
    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. Read More

    Proliposome Powders for the Generation of Liposomes: the Influence of Carbohydrate Carrier and Separation Conditions on Crystallinity and Entrapment of a Model Antiasthma Steroid.
    AAPS PharmSciTech 2017 Jul 11. Epub 2017 Jul 11.
    Pharmaceutical Sciences Section, College of Pharmacy, Qatar University, P.O. Box 2713, Doha, Qatar.
    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. Read More

    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(®) 150 and 300 μg.
    AAPS PharmSciTech 2017 Jul 10. Epub 2017 Jul 10.
    Department of Pharmacy and Pharmaceutical Sciences, University of Huddersfield, Queensgate, Huddersfield, HD1 3DH, UK.
    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. Indacaterol 150 and 300 μg contain equal amounts of lactose per carrier. Read More

    Aqueous Polymer Dispersion Coating Used for Osmotic Pump Tablets: Membrane Property Investigation and IVIVC Evaluation.
    AAPS PharmSciTech 2017 Jul 10. Epub 2017 Jul 10.
    Department of Pharmaceutics, School of Pharmaceutical science, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
    The objective of this study was to investigate the fundamental properties of propranolol hydrochloride osmotic pump tablets coated by aqueous polymer dispersion, simultaneously exploring the in vitro and in vivo correlation of the tablet. The physicochemical properties and parameters of aqueous polymer dispersion membranes (SEM, water uptake, and water vapor transmission coefficient) were investigated. In addition, the release behavior and the in vitro release and in vivo absorption profiles of the tablets coated by aqueous polymer dispersion were investigated by comparing with propranolol hydrochloride osmotic pump tablets coated by an organic solvent. Read More

    Enhanced Ungual Permeation of Terbinafine HCl Delivered Through Liposome-Loaded Nail Lacquer Formulation Optimized by QbD Approach.
    AAPS PharmSciTech 2017 Jul 5. Epub 2017 Jul 5.
    Drug Discovery Lab, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER)-Ahmedabad, Opp. To Air force Station, Palaj, Gandhinagar, Gujarat, 382355, India.
    The present investigation focused on developing, optimizing, and evaluating a novel liposome-loaded nail lacquer formulation for increasing the transungual permeation flux of terbinafine HCl for efficient treatment of onychomycosis. A three-factor, three-level, Box-Behnken design was employed for optimizing process and formulation parameters of liposomal formulation. Liposomes were formulated by thin film hydration technique followed by sonication. Read More

    Preparation of a Sustained-Release Nebulized Aerosol of R-terbutaline Hydrochloride Liposome and Evaluation of Its Anti-asthmatic Effects via Pulmonary Delivery in Guinea Pigs.
    AAPS PharmSciTech 2017 Jul 5. Epub 2017 Jul 5.
    Institute of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou, China.
    An aerosolized liposome formulation for the pulmonary delivery of an anti-asthmatic medication was developed. Asthma treatment usually requires frequent administration of medication for a sustained bronchodilator response. Liposomes are known for their sustained drug release capability and thus would be a suitable delivery system for prolonging the therapeutic effect of anti-asthmatic medication. Read More

    Association of Silver Nanoparticles and Curcumin Solid Dispersion: Antimicrobial and Antioxidant Properties.
    AAPS PharmSciTech 2017 Jul 5. Epub 2017 Jul 5.
    LaBNUS-Biomaterials and Nanotechnology Laboratory, University of Sorocaba, Sorocaba, SP, Brazil.
    The last century, more precisely after 1945, was marked by major advances in the treatment of infectious diseases which promoted a decrease in mortality and morbidity. Despite these advances, currently the development of antimicrobial resistance has been growing drastically and therefore there is a pressing need to search for new compounds. Silver nanoparticles (AgNps) have been demonstrating good antimicrobial activity against different bacteria, viruses, and fungi. Read More

    Topical Delivery of Coumestrol from Lipid Nanoemulsions Thickened with Hydroxyethylcellulose for Antiherpes Treatment.
    AAPS PharmSciTech 2017 Jul 5. Epub 2017 Jul 5.
    Programa de Pós-graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Av. Ipiranga 2752, Porto Alegre, 90610-000, Brazil.
    We have recently shown that coumestrol, an isoflavonoid-like compound naturally occurring in soybeans, alfafa, and red clover, inhibited Herpes Simplex Virus types 1 (HSV-1) and 2 (HSV-2) replication. In this study, we designed coumestrol formulations in an attempt to enable its topical delivery to mucosa tissues. Physicochemical and microscopic examinations suggested that coumestrol was efficiently incorporated in positively-charged nanoemulsions dispersed in a hydroxyethylcellulose gel. Read More

    Antiproliferative Activity and VEGF Expression Reduction in MCF7 and PC-3 Cancer Cells by Paclitaxel and Imatinib Co-encapsulation in Folate-Targeted Liposomes.
    AAPS PharmSciTech 2017 Jul 5. Epub 2017 Jul 5.
    Laboratory of Pharmaceutical Nanotechnology and Drug Delivery Systems, School of Pharmacy, Federal University of Goiás, Goiânia, Goiás, Brazil.
    Co-encapsulation of anticancer drugs paclitaxel and imatinib in nanocarriers is a promising strategy to optimize cancer treatment. Aiming to combine the cytotoxic and antiangiogenic properties of the drugs, a liposome formulation targeted to folate receptor co-encapsulating paclitaxel and imatinib was designed in this work. An efficient method was optimized for the synthesis of the lipid anchor DSPE-PEG(2000)-folic acid (FA). Read More

    Development and In Vitro-In Vivo Characterization of Chronomodulated Pulsatile Delivery Formulation of Terbutaline Sulphate by Box-Behnken Statistical Design.
    AAPS PharmSciTech 2017 Jun 30. Epub 2017 Jun 30.
    Ch. Devilal College of Pharmacy, Jagadhri, Yamunanagar, Haryana, India.
    In the present study, we have designed a press-coated pulsatile delivery tablet (PDT) of Terbutaline sulphate (TS) intended for prevention of early-morning asthma attacks. The formulation is capable of giving burst release of drug after 6 h of lag time. In this study, a press-coating technique was employed to coat a fast-release core tablet containing TS with a polymeric release retarding coat comprising of ethyl cellulose, HPMC K15M and Carbopol 971P. Read More

    Sucrose Octaacetate Chemical Kinetics and Shelf Lives at Various Formulation pHs.
    AAPS PharmSciTech 2017 Jun 23. Epub 2017 Jun 23.
    Department of Pharmaceutical Sciences, Campbell University College of Pharmacy & Health Sciences, Buies Creek, North Carolina, USA.
    Developing pediatric friendly dosage forms is a high priority worldwide. Sucrose octaacetate (SOA) has been recommended for use as a surrogate for bitter tasting active pharmaceutical ingredients. Even though SOA has found a number of human use applications and has been employed for decades, there are no rigorous chemical kinetic studies reported. Read More

    Identification of Particles in Raw Materials.
    AAPS PharmSciTech 2017 Jun 23. Epub 2017 Jun 23.
    , 11 Deer Park Drive, Suite 201, Monmouth Junction New Jersey, 08852, USA.
    Raw materials need to be of a certain quality with respect to physical and chemical composition. They also need to have no contaminants in the form of particles because these could get into the product or indicate the raw materials are not pure enough to make a good quality product. When particles are found, it is important to identify their chemical and elemental composition to correct any process errors that can cause them and to have acceptable quality of the final product. Read More

    Effective Skin Cancer Treatment by Topical Co-delivery of Curcumin and STAT3 siRNA Using Cationic Liposomes.
    AAPS PharmSciTech 2017 Jun 21. Epub 2017 Jun 21.
    Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana, 500078, India.
    The aim of the present study was to evaluate the effectiveness of iontophoretic co-delivery of curcumin and anti-STAT3 siRNA using cationic liposomes against skin cancer. Curcumin was encapsulated in DOTAP-based cationic liposomes and then complexed with STAT3 siRNA. This nanocomplex was characterized for the average particle size, zeta-potential, and encapsulation efficiency. Read More

    Feasibility of Focused Beam Reflectance Measurement (FBRM) for Analysis of Pharmaceutical Suspensions in Preclinical Development.
    AAPS PharmSciTech 2017 Jun 21. Epub 2017 Jun 21.
    Material and Analytical Sciences, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut, 06877, USA.
    This study examined the use of focused beam reflectance measurement (FBRM) for qualitative and quantitative analysis of pharmaceutical suspensions with particular application to toxicology supply preparations for use in preclinical studies. Aqueous suspensions of ibuprofen were used as prototype formulations. Initial experiments were conducted to examine the effects of operational conditions including FBRM probe angle, probe location, and mixing (method and rate of mixing) on the FBRM analysis. Read More

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