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    2506 results match your criteria AAPS PharmSciTech[Journal]

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    Enhancing the Therapeutic Efficacy of Tamoxifen Citrate Loaded Span-Based Nano-Vesicles on Human Breast Adenocarcinoma Cells.
    AAPS PharmSciTech 2018 Feb 22. Epub 2018 Feb 22.
    Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Cairo, Egypt.
    Serious adverse effects and low selectivity to cancer cells are the main obstacles of long term therapy with Tamoxifen (Tmx). This study aimed to develop Tmx-loaded span-based nano-vesicles for delivery to malignant tissues with maximum efficacy. The effect of three variables on vesicle size (Y), zeta potential (Y), entrapment efficiency (Y) and the cumulative percent release after 24 h (Y) were optimized using Box-Behnken design. Read More

    Enhancement of Dissolution and Skin Permeability of Pentazocine by Proniosomes and Niosomal Gel.
    AAPS PharmSciTech 2018 Feb 22. Epub 2018 Feb 22.
    Department of Pharmacy, COMSATS Institute of Science and Technology, Abbottabad, Khyber Pakhtunkhwa, 22010, Pakistan.
    Proniosomes (PN) are the dry water-soluble carrier systems that may enhance the oral bioavailability, stability, and topical permeability of therapeutic agents. The low solubility and low oral bioavailability due to extensive first pass metabolism make Pentazocine as an ideal candidate for oral and topical sustained release delivery. The present study was aimed to formulate the PNs by quick slurry method that are converted to niosomes (liquid dispersion) by hydration, and subsequently formulated to semisolid niosomal gel. Read More

    In Vitro Characterization and Evaluation of the Cytotoxicity Effects of Nisin and Nisin-Loaded PLA-PEG-PLA Nanoparticles on Gastrointestinal (AGS and KYSE-30), Hepatic (HepG2) and Blood (K562) Cancer Cell Lines.
    AAPS PharmSciTech 2018 Feb 22. Epub 2018 Feb 22.
    Department of Biology, Faculty of Science, University of Mohaghegh Ardabili, Daneshgah St, Ardabil, 11367-56199, Iran.
    The aim of this study was an in vitro evaluation and comparison of the cytotoxic effects of free nisin and nisin-loaded PLA-PEG-PLA nanoparticles on gastrointestinal (AGS and KYSE-30), hepatic (HepG2), and blood (K562) cancer cell lines. To create this novel anti-cancer drug delivery system, the nanoparticles were synthesized and then loaded with nisin. Subsequently, their biocompatibility, ability to enter cells, and physicochemical properties, including formation, size, and shape, were studied using hemolysis, fluorescein isothiocyanate (FITC), Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), and scanning electron microscopy (SEM), respectively. Read More

    Inhalable Levofloxacin Liposomes Complemented with Lysozyme for Treatment of Pulmonary Infection in Rats: Effective Antimicrobial and Antibiofilm Strategy.
    AAPS PharmSciTech 2018 Feb 20. Epub 2018 Feb 20.
    Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai, 400098, India.
    Treatment of bacterial infections becomes increasingly complicated due to increasing bacterial resistance and difficulty in developing new antimicrobial agents. Emphasis should be laid on improvising the existing treatment modalities. We studied the improved antimicrobial and antibiofilm activity of levofloxacin (LFX) and lysozyme (LYS) in microbiological studies. Read More

    Improving Properties of Albendazole Desmotropes by Supramolecular Systems with Maltodextrin and Glutamic Acid.
    AAPS PharmSciTech 2018 Feb 20. Epub 2018 Feb 20.
    Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina.
    Albendazole, an effective broad-spectrum anthelmintic agent, showed unpredictable therapeutic response caused by poor water solubility and slow dissolution rate. Then, novel binary and multicomponent supramolecular systems of two different solid forms of albendazole (I and II) with maltodextrin alone or with glutamic acid were studied as an alternative to improve the oral bioavailability of albendazole. The interactions and effects on the properties of albendazole were studied in solution and solid state. Read More

    Delivery Considerations of Highly Viscous Polymeric Fluids Mimicking Concentrated Biopharmaceuticals: Assessment of Injectability via Measurement of Total Work Done "W".
    AAPS PharmSciTech 2018 Feb 20. Epub 2018 Feb 20.
    School of Pharmacy, Temple University, 3307 North Broad St., Philadelphia, Pennsylvania, 19140, USA.
    An account is given of the recent development of the highly viscous complex biopharmaceuticals in relation to syringeability and injectability. The specific objective of this study is to establish a convenient method to examine problem of the injectability for the needle-syringe-formulation system when complex formulations with diverse viscosities are used. This work presents the inter-relationship between needle size, syringe volume, viscosity, and injectability of polymeric solutions having typical viscosities encountered in concentrated biologics, by applying a constant probe crosshead speed on the plunger-syringe needle assembly and continuously recording the force-distance profiles. Read More

    Design and Characterization of Topical Formulations: Correlations Between Instrumental and Sensorial Measurements.
    AAPS PharmSciTech 2018 Feb 20. Epub 2018 Feb 20.
    School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Avenida do Café, s/n - Monte Alegre, Ribeirão Preto, SP, 14040-903, Brazil.
    The interaction between cosmetic emulsions and the skin's surface is an important factor to consider in the development of topical formulations. Two important ingredients in cosmetic formulations are waxes and polymers. The physical and mechanical properties of formulations directly impact the interface skin-formulation. Read More

    Artificial Lipid Membrane Permeability Method for Predicting Intestinal Drug Transport: Probing the Determining Step in the Oral Absorption of Sulfadiazine; Influence of the Formation of Binary and Ternary Complexes with Cyclodextrins.
    AAPS PharmSciTech 2018 Feb 15. Epub 2018 Feb 15.
    Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA) CONICET-UNC and Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA, Córdoba, Argentina.
    We propose an in vitro permeability assay by using a modified lipid membrane to predict the in vivo intestinal passive permeability of drugs. Two conditions were tested, one with a gradient pH (pH 5.5 donor/pH 7. Read More

    The Role of Excipients in the Stability of Triamcinolone Acetonide in Ointments.
    AAPS PharmSciTech 2018 Feb 15. Epub 2018 Feb 15.
    Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, 3584 CG, Utrecht, the Netherlands.
    Degradation of triamcinolone acetonide (TCA) in an ointment was investigated. TCA appeared to be concentrated in propylene glycol (PG) which in turn is dispersed in a lanolin-petrolatum mixture. Two predominant degradation products were identified: a 21-aldehyde and a 17-carboxylic acid. Read More

    A Novel Approach for Dry Powder Coating of Pellets with Ethylcellulose. Part II: Evaluation of Caffeine Release.
    AAPS PharmSciTech 2018 Feb 13. Epub 2018 Feb 13.
    Department of Pharmacy and BioTechnology, University of Bologna, Via S. Donato 19/2, 40127, Bologna, Italy.
    The objective of this study was to assess the efficacy and the capability of a novel ethylcellulose-based dry-coating system to obtain prolonged and stable release profiles of caffeine-loaded pellets. Lauric and oleic acids at a suitable proportion were used to plasticize ethylcellulose. The effect of coating level, percentage of drug loading, inert core particle size, and composition of the coating formulation including the anti-sticking agent on the drug release profile were fully investigated. Read More

    Performance of the Population Bioequivalence (PBE) Statistical Test Using an IPAC-RS Database of Delivered Dose from Metered Dose Inhalers.
    AAPS PharmSciTech 2018 Feb 12. Epub 2018 Feb 12.
    Pharmaceutical Practice Group, Drinker Biddle & Reath LLP, 1500 K Street, N.W., Suite 1100, Washington, District of Columbia, 20005-1209, USA.
    This article reports performance characteristics of the population bioequivalence (PBE) statistical test recommended by the US Food and Drug Administration (FDA) for orally inhaled products. A PBE Working Group of the International Pharmaceutical Aerosol Consortium on Regulation and Science (IPAC-RS) assembled and considered a database comprising delivered dose measurements from 856 individual batches across 20 metered dose inhaler products submitted by industry. A review of the industry dataset identified variability between batches and a systematic lifestage effect that was not included in the FDA-prescribed model for PBE. Read More

    Preparation of Controlled-Release Particles Based on Spherical Porous Silica Used as the Drug Carrier by the Dry Coating Method.
    AAPS PharmSciTech 2018 Feb 12. Epub 2018 Feb 12.
    Department of Pharmaceutical Technology, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama, Ehime, 790-8578, Japan.
    A controlled-release formulation is a dosage form that could improve a patient's quality of life by reducing the frequency of administration, while ensuring the continued effect of the medicine and reducing the side effects. To prepare these controlled-release particles, a wet coating method in which a drug is coated with a controlled-release material using water or an organic solvent is used, but with this method, the coating process is very time-consuming and requires large amounts of energy for the drying phase. In addition, contact with water or an organic solvent may cause problems such as alteration of the drug. Read More

    Comparative Study of Glyceryl Behenate or Polyoxyethylene 40 Stearate-Based Lipid Carriers for Trans-Resveratrol Delivery: Development, Characterization and Evaluation of the In Vitro Tyrosinase Inhibition.
    AAPS PharmSciTech 2018 Feb 5. Epub 2018 Feb 5.
    School of Pharmaceutical Sciences, Campus Araraquara, Department of Drugs and Medicines, UNESP-São Paulo State University, Rodovia Araraquara-Jau, km 1, Araraquara, São Paulo, 14800-903, Brazil.
    Trans-resveratrol (RSV) is a natural compound with several properties, such as the ability to inhibit the tyrosinase enzyme, with potential application as a skin-lightning agent and for the treatment of skin disorders associated with hyperpigmentation and melanogenesis. However, the drug faces several drawbacks which altogether limit its therapeutic application. Thus, drug loading into nanocarriers emerge as an alternative to circumvent these problems. Read More

    Formulation and Characterization of Fast-Dissolving Sublingual Film of Iloperidone Using Box-Behnken Design for Enhancement of Oral Bioavailability.
    AAPS PharmSciTech 2018 Feb 2. Epub 2018 Feb 2.
    Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Vile Parle (W), Mumbai, Maharashtra, 400056, India.
    Iloperidone is a second-generation antipsychotic drug which is used for the treatment of schizophrenia and has very low aqueous solubility and bioavailability. This drug also undergoes first-pass metabolism. The aim of this work is to formulate fast-dissolving sublingual films of iloperidone to improve its bioavailability. Read More

    Risk Assessment Integrated QbD Approach for Development of Optimized Bicontinuous Mucoadhesive Limicubes for Oral Delivery of Rosuvastatin.
    AAPS PharmSciTech 2018 Jan 31. Epub 2018 Jan 31.
    Department of Pharmaceutics, Faculty of Pharmacy, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062, India.
    Statins are widely prescribed for hyperlipidemia, cancer, and Alzheimer's disease but are facing some inherent challenges such as low solubility and drug loading, higher hepatic metabolism, as well as instability at gastric pH. So, relatively higher circulating dose, required for exerting the therapeutic benefits, leads to dose-mediated severe toxicity. Furthermore, due to low biocompatibility, high toxicity, and other regulatory caveats such as product conformity, reproducibility, and stability of conventional formulations as well as preferentially higher bioabsorption of lipids in their favorable cuboidal geometry, enhancement in in vivo biopharmaceutical performance of Rosuvastatin could be well manifested in Quality by Design (QbD) integrated cuboidal-shaped mucoadhesive microcrystalline delivery systems (Limicubes). Read More

    Formulation and Evaluation of Organogels Containing Hyaluronan Microparticles for Topical Delivery of Caffeine.
    AAPS PharmSciTech 2018 Jan 29. Epub 2018 Jan 29.
    Faculty of Pharmacy, Department of Pharmaceutical Technology, Ege University, 35100, Izmir, Turkey.
    Cellulite is a dermal disorder including the extracellular matrix, the lymphatic and microcirculatory systems and the adipose tissue. Caffeine is used as the active moiety depending its preventive effect on localization of fat in the cellular structure. Hyaluronic acid (hyaluronan-HA) is a natural constituent of skin that generates formation and poliferation of new cells having a remarkable moisturizing ability. Read More

    Retraction Note: Development and In Vitro-In Vivo Characterization of Chronomodulated Pulsatile Delivery Formulation of Terbutaline Sulphate by Box-Behnken Statistical Design.
    AAPS PharmSciTech 2018 Jan 29. Epub 2018 Jan 29.
    Ch. Devilal College of Pharmacy, Jagadhri, Yamunanagar, Haryana, India.
    This article has been retracted by the journal because the editors have clear evidence that the scientific findings in this article are unreliable. Read More

    Micronized Zaleplon Delivery via Orodispersible Film and Orodispersible Tablets.
    AAPS PharmSciTech 2018 Jan 19. Epub 2018 Jan 19.
    Department of Pharmaceutics and Drug Delivery, The University of Mississippi, University, Oxford, MS, 38677, USA.
    The following research study focuses on improving the solubility of zaleplon (BCS class II drug) via micronization technique in order to enhance its oral delivery in orodispersible formulations. Zaleplon along with a surfactant solution was micronized by ultrasonication. The micronization process reduced the particle size of the crystalline drug about six-fold from its original size of 155. Read More

    Controlled Release of the Nimodipine-Loaded Self-Microemulsion Osmotic Pump Capsules: Development and Characterization.
    AAPS PharmSciTech 2018 Jan 16. Epub 2018 Jan 16.
    Department of Pharmaceutics, School of Pharmacy, Guangzhou Higher Education Mega Center, Guangdong Pharmaceutical University, No. 280 Waihuandong Road, Guangzhou, 510006, China.
    The present study was intended to develop a controlled released osmotic pump capsule based on Nimodipine (NM)-loaded self-microemulsifying drug delivery systems (SMEDDSs) in order to improve the low oral bioavailability of NM. To optimize the NM-loaded SMEDDS composition, the experiments of NM solubility in different oils, the pseudo-ternary phase diagram experiments and the different drug loading experiments were conducted in the preliminary screening studies. Controlled release of NM required an osmotic pump capsule comprising a coated semi-permeable capsule shell, plasticizer, and pore-forming agent. Read More

    Nanolipid Gel of an Antimycotic Drug for Treating Vulvovaginal Candidiasis-Development and Evaluation.
    AAPS PharmSciTech 2018 Jan 16. Epub 2018 Jan 16.
    Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai, 400098, India.
    This paper focuses on the development and evaluation of mucoadhesive vaginal gel of fluconazole using nanolipid carriers to enhance tissue deposition in treating vulvovaginal candidiasis. Treatment of vulvovaginal candidiasis includes antimycotic agents prescribed for 1 to 7 days or longer, in relapse either orally or topically. The delivery of fluconazole as nanolipid carriers in vaginal gel can be proposed as suitable alternative to the existing conventional formulations to improve the patient acceptability, compliance and localized drug action. Read More

    Facile Synthesis of Chitosan Capped Mesoporous Silica Nanoparticles: A pH Responsive Smart Delivery Platform for Raloxifene Hydrochloride.
    AAPS PharmSciTech 2018 Jan 16. Epub 2018 Jan 16.
    Faculty of Pharmacy, Centre of Relevance and Excellence in New Drug Delivery System, Government of India, The Maharaja Sayajirao University of Baroda, Kalabhavan Campus, Vadodara, 390002, India.
    An encapsulation of model drug raloxifene hydrochloride (RAL) inside the chitosan decorated pH responsive mesoporous system has a greater potential for accumulating in the tumor cells. The present study involves synthesis of surface modified mesoporous silica nanoparticles (MSN) with the aim of achieving pH sensitive drug delivery system. A silanol skeleton of MSN has been productively modified to amine intermediate which served as a firm platform to adapt chitosan grafted assembly and systematically evaluated. Read More

    Effect of Moisture Content of Chitin-Calcium Silicate on Rate of Degradation of Cefotaxime Sodium.
    AAPS PharmSciTech 2018 Jan 16. Epub 2018 Jan 16.
    Pharmaceutical Technology Department, Faculty of Pharmacy, Jordan University of Science and Technology, P.O.Box 3030, Irbid, 22110, Jordan.
    Assessment of incompatibilities between active pharmaceutical ingredient and pharmaceutical excipients is an important part of preformulation studies. The objective of the work was to assess the effect of moisture content of chitin calcium silicate of two size ranges (two specific surface areas) on the rate of degradation of cefotaxime sodium. The surface area of the excipient was determined using adsorption method. Read More

    Methotrexate Aspasomes Against Rheumatoid Arthritis: Optimized Hydrogel Loaded Liposomal Formulation with In Vivo Evaluation in Wistar Rats.
    AAPS PharmSciTech 2018 Jan 16. Epub 2018 Jan 16.
    Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, 700032, India.
    Aspasomes of methotrexate with antioxidant, ascorbyl palmitate, were developed and optimized using factorial design by varying parameters such as lipid molar ratio, drug to lipid molar ratio, and type of hydration buffer for transdermal delivery for disease modifying activity in rheumatoid arthritis (RA). Aspasomes were characterized by drug-excipients interaction, particle size analysis, determination of zeta potential, entrapment efficiency, and surface properties. The best formulation was loaded into hydrogel for evaluation of in vitro drug release and tested in vivo against adjuvant induced arthritis model in wistar rats, by assessing various physiological, biochemical, hematological, and histopathological parameters. Read More

    New Strategies for Improving the Development and Performance of Amorphous Solid Dispersions.
    AAPS PharmSciTech 2018 Jan 16. Epub 2018 Jan 16.
    Division of Pharmaceutics, College of Pharmacy, the University of Texas at Austin, 2409 University Avenue, A1920, Austin, Texas, 78712, USA.
    The understanding of amorphous solid dispersions has grown significantly in the past decade. This is evident from the number of approved commercial amorphous solid dispersion products. While amorphous formulation is considered an enabling technology, it has become the norm for formulating poorly soluble compounds. Read More

    Correction to: Promising Antibacterial Effects of Silver Nanoparticle-Loaded Tea Tree Oil Nanoemulsion: a Synergistic Combination Against Resistance Threat.
    AAPS PharmSciTech 2018 Jan 11. Epub 2018 Jan 11.
    Department of Medical Nanotechnology, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran.
    With regrets, there is an error in the name of one of the authors which has only been noticed after publication. Read More

    Theoretical and Experimental Studies of the Controlled Release of Tetracycline Incorporated into Bioactive Glasses.
    AAPS PharmSciTech 2018 Jan 9. Epub 2018 Jan 9.
    Departamento de Química, ICEx, Universidade Federal de Minas Gerais, UFMG, Av. Antônio Carlos, 6627, Belo Horizonte, MG, (31.270-901), Brazil.
    Several authors have studied the release profile of drugs incorporated in different devices. However, to the best of our knowledge, although many studies have been done on the release of tetracycline, in these release devices, no study has investigated if the released compound is actually the tetracycline, or, instead, a degraded product. This approach is exploited here. Read More

    Structural Elucidation of Poloxamer 237 and Poloxamer 237/Praziquantel Solid Dispersions: Impact of Poly(Vinylpyrrolidone) over Drug Recrystallization and Dissolution.
    AAPS PharmSciTech 2018 Jan 8. Epub 2018 Jan 8.
    CQE, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001, Lisbon, Portugal.
    Praziquantel (PZQ) is the recommended, effective, and safe treatment against all forms of schistosomiasis. Solid dispersions (SDs) in water-soluble polymers have been reported to increase solubility and bioavailability of poorly water-soluble drugs like PZQ, generally due to the amorphous form stabilization. In this work, poloxamer (PLX) 237 and poly(vinylpyrrolidone) (PVP) K30 were evaluated as potential carriers to revert PZQ crystallization. Read More

    Enhancement of In Vivo Efficacy and Oral Bioavailability of Aripiprazole with Solid Lipid Nanoparticles.
    AAPS PharmSciTech 2018 Jan 8. Epub 2018 Jan 8.
    University Institute of Pharmaceutical Sciences, Panjab University, Sector-14, Chandigarh, India.
    Aripiprazole (ARP), a second-generation or atypical antipsychotic, is poorly soluble and undergoes extensive hepatic metabolism and P-glycoprotein efflux which lead to reduced in vivo efficacy and increased dose-related side effects. To enhance in vivo efficacy and oral bioavailability of aripiprazole, aripiprazole-loaded solid lipid nanoparticles (SLNs) were developed using tristearin as solid lipid. Tween 80 and sodium taurocholate were used as surfactants to prepare SLNs using microemulsification method. Read More

    Preparation and Evaluation of Progesterone Nanocrystals to Decrease Muscle Irritation and Improve Bioavailability.
    AAPS PharmSciTech 2018 Jan 8. Epub 2018 Jan 8.
    State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing, 100850, China.
    Progesterone (PG) is a crucial immunomodulatory agent during early pregnancy, and nowadays PG oil-based injection (PG/OI) has a huge market all over the world. However, PG/OI may accumulate the local muscle and further cause irritations after long-term administration. In this study, PG nanocrystals (PG/NCs) injection was developed to decrease muscle toxicity. Read More

    A Scale-up Approach for Film Coating Process Based on Surface Roughness as the Critical Quality Attribute.
    AAPS PharmSciTech 2018 Jan 5. Epub 2018 Jan 5.
    Department of Pharmaceutical Engineering, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka, 422-8526, Japan.
    Scale-up approaches for film coating process have been established for each type of film coating equipment from thermodynamic and mechanical analyses for several decades. The objective of the present study was to establish a versatile scale-up approach for film coating process applicable to commercial production that is based on critical quality attribute (CQA) using the Quality by Design (QbD) approach and is independent of the equipment used. Experiments on a pilot scale using the Design of Experiment (DoE) approach were performed to find a suitable CQA from surface roughness, contact angle, color difference, and coating film properties by terahertz spectroscopy. Read More

    Control Strategy for Small Molecule Impurities in Antibody-Drug Conjugates.
    AAPS PharmSciTech 2018 Jan 4. Epub 2018 Jan 4.
    AbbVie Inc., 1 North Waukegan Rd, North Chicago, Illinois, 60064-1802, USA.
    Antibody-drug conjugates (ADCs) are an emerging class of biopharmaceuticals. As such, there are no specific guidelines addressing impurity limits and qualification requirements. The current ICH guidelines on impurities, Q3A (Impurities in New Drug Substances), Q3B (Impurities in New Drug Products), and Q6B (Specifications: Test Procedures and Acceptance Criteria for Biotechnological/Biological Products) do not adequately address how to assess small molecule impurities in ADCs. Read More

    Screen for Inhibitors of Crystal Growth to Identify Desirable Carriers for Amorphous Solid Dispersions Containing Felodipine.
    AAPS PharmSciTech 2018 Jan 4. Epub 2018 Jan 4.
    Laboratory of Pharmaceutical Crystal Engineering & Technology, School of Pharmacy, East China University of Science and Technology, 363#, No. 130, Meilong Rd, Shanghai, 200237, China.
    The solvent-shift method was used to identify appropriate polymers that inhibit the growth of felodipine crystals by monitoring particle size in supersaturated drug solutions in the presence of different polymers. We speculated that there would be an intermolecular interaction between the selected polymer (zein) and felodipine by extrapolating the inhibitory effect on crystal growth and then used the selected polymer as a carrier to prepare solid dispersions. The formulations were characterized by crystalline properties, thermodynamics of mixing, dissolution behavior, and physical stability. Read More

    Hydrogels Containing Antibiofilm and Antimicrobial Agents Beneficial for Biofilm-Associated Wound Infection: Formulation Characterizations and In vitro Study.
    AAPS PharmSciTech 2017 Dec 26. Epub 2017 Dec 26.
    Center for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, 50300, Kuala Lumpur, Malaysia.
    Bacterial biofilm which adheres onto wound surface is shown to be impervious to antibiotics and this in turn delays wound healing. Previous studies showed that antibiofilm agents such as xylitol and ethylenediaminetetraacetic acid (EDTA) prevent bacterial adherence onto surfaces. Formulation of a wound dressing containing antibiofilm agents may be a plausible strategy in breaking the biofilm on wound surfaces and at the same time increase the efficacy of the antibiotic. Read More

    ω-3 Fatty Acid Synergized Novel Nanoemulsifying System for Rosuvastatin Delivery: In Vitro and In Vivo Evaluation.
    AAPS PharmSciTech 2017 Dec 19. Epub 2017 Dec 19.
    Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Rae Bareli Road, Lucknow, 226025, India.
    The present study was undertaken to improve rosuvastatin (RSV) bioavailability and pharmacological response through formation of SNES using Perilla frutescens oil as lipid carrier. The composition of oil was estimated by fatty acid methyl ester (FAME) analysis using gas chromatography. Solubility of RSV in Perilla frutescens oil and Cremophor EL was 25. Read More

    Photodegradation of Moxifloxacin Hydrochloride Solutions under Visible Light Irradiation: Identification of Products and the Effect of pH on their Formation.
    AAPS PharmSciTech 2017 Dec 18. Epub 2017 Dec 18.
    Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, China.
    The photodegradation study is essential for the phototoxicity assessment of fluoroquinolones. Various LC-MS techniques and ultraviolet (UV) lamp irradiation conditions have been used for the identification of their photodegradation products. In this study, visible light (400-760 nm) lamp irradiation was selected for the photodegradation of moxifloxacin (MOXI) hydrochloride solutions. Read More

    Antioxidant-Based Eutectics of Irbesartan: Viable Multicomponent Forms for the Management of Hypertension.
    AAPS PharmSciTech 2017 Dec 15. Epub 2017 Dec 15.
    University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies, Panjab University, Sector-14, Chandigarh, 160 014, India.
    The present research work highlights the development of multicomponent solid form of the antihypertensive drug irbesartan (IRB) to improve its biopharmaceutical attributes. Mechanochemical synthesis of a new solid form of IRB with coformers having antioxidant properties (syringic acid, nicotinic acid, and ascorbic acid) resulted into three eutectic mixtures (EMs). Formation of eutectic was ascertained by differential scanning calorimetry whereas exact stoichiometry (50/50% w/w) was established by phase diagram and Tamman's triangle. Read More

    Lipid A adjuvanted Chylomicron Mimicking Solid Fat Nanoemulsions for Immunization Against Hepatitis B.
    AAPS PharmSciTech 2017 Dec 14. Epub 2017 Dec 14.
    SLT Institute of Pharmaceutical sciences, Guru Ghasidas Vishwavidyalaya, Koni, Bilaspur, CG, 495009, India.
    Traditional parenteral recombinant hepatitis B virus (HBV) vaccines have effectively reduced the disease burden despite being able to induce seroprotective antibody titers in 5-10% vaccinated individuals (non-responders). Moreover, an estimated 340 million chronic HBV cases are in need of treatment. Development of safe, stable, and more effective hepatitis B vaccine formulation would address these challenges. Read More

    Combined Poly(Lactide-Co-Glycolide) Microspheres Containing Diphtheria Toxoid for a Single-shot Immunization.
    AAPS PharmSciTech 2017 Dec 13. Epub 2017 Dec 13.
    College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul, 06974, South Korea.
    To develop a single-shot vaccine containing diphtheria toxoid (DT) with a sufficient immune response, poly(lactide-co-glycolide) (PLGA) microspheres were prepared by water-in-oil-in-water double emulsification and solvent extraction techniques using low or high-molecular-weight PLGA (LMW-MS or HMW-MS). Stearic acid (SA) was introduced to HMW-MS (HMW/SA-MS) as a release modulator. Mean particle sizes (dvs, μm) varied between the prepared microspheres, with LMW-MS, HMW-MS, and HMW/SA-MS having the sizes of 29. Read More

    Promising Antibacterial Effects of Silver Nanoparticle-Loaded Tea Tree Oil Nanoemulsion: a Synergistic Combination Against Resistance Threat.
    AAPS PharmSciTech 2017 Dec 7. Epub 2017 Dec 7.
    Department of Medical Nanotechnology, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran.
    Highly resistant pathogens may be developed in patients with immune disorders after prolonged exposure to antibiotics, a growing threat worldwide. In order to overcome these problems, this study introduces a new class of engineered nanosystems comprising of tea tree oil nanoemulsion (TTO NE) loaded with Ag nanoparticles (NPs). Silver shows a strong toxicity towards a wide range of microorganisms. Read More

    Application of Fluorescence Emission for Characterization of Albendazole and Ricobendazole Micellar Systems: Elucidation of the Molecular Mechanism of Drug Solubilization Process.
    AAPS PharmSciTech 2017 Dec 7. Epub 2017 Dec 7.
    IQUIR-CONICET, Suipacha 570, S2002LRK, Rosario, Argentina.
    Albendazole (ABZ) and ricobendazole (RBZ) are referred to as class II compounds in the Biopharmaceutical Classification System. These drugs exhibit poor solubility, which profoundly affects their oral bioavailability. Micellar systems are excellent pharmaceutical tools to enhance solubilization and absorption of poorly soluble compounds. Read More

    Fabrication of Tip-Dissolving Microneedles for Transdermal Drug Delivery of Meloxicam.
    AAPS PharmSciTech 2017 Dec 7. Epub 2017 Dec 7.
    School of Pharmacy and Medical Technology, Putian University, 351100, Fujian, China.
    Dissolving microneedles (MNs) offered a simple, minimally invasive method for meloxicam (MX) delivery to the skin. However, the fabrication of dissolving MNs still faced some challenges, such as significant time consumption, loss of drug activity, and difficulty in regulating MN drug loading. To address these issues, we developed the tip-dissolving (TD) MNs. Read More

    Soy Protein Microparticles for Enhanced Oral Ibuprofen Delivery: Preparation, Characterization, and In Vitro Release Evaluation.
    AAPS PharmSciTech 2017 Dec 6. Epub 2017 Dec 6.
    Laboratoire de Chimie Agro-industrielle (LCA), Université de Toulouse, INRA, INPT, Toulouse, France.
    The objective of this work was to evaluate soy protein isolate (SPI) and acylated soy protein (SPA) as spray-drying encapsulation carriers for oral pharmaceutical applications. SPI acylation was performed by the Schotten-Baumann reaction. SPA, with an acylation rate of 41%, displayed a decrease in solubility in acidic conditions, whereas its solubility was unaffected by basic conditions. Read More

    A Science and Risk-Based Pragmatic Methodology for Blend and Content Uniformity Assessment.
    AAPS PharmSciTech 2017 Dec 6. Epub 2017 Dec 6.
    Apotex Inc., 150 Signet Drive, Toronto, Ontario, M9L 1T9, Canada.
    This paper describes a pragmatic approach that can be applied in assessing powder blend and unit dosage uniformity of solid dose products at Process Design, Process Performance Qualification, and Continued/Ongoing Process Verification stages of the Process Validation lifecycle. The statistically based sampling, testing, and assessment plan was developed due to the withdrawal of the FDA draft guidance for industry "Powder Blends and Finished Dosage Units-Stratified In-Process Dosage Unit Sampling and Assessment." This paper compares the proposed Grouped Area Variance Estimate (GAVE) method with an alternate approach outlining the practicality and statistical rationalization using traditional sampling and analytical methods. Read More

    Development of Itraconazole Tablets Containing Viscous KinetiSol® Solid Dispersions: In Vitro and In Vivo Analysis in Dogs.
    AAPS PharmSciTech 2017 Nov 30. Epub 2017 Nov 30.
    Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, A1920, Austin, Texas, 78712, USA.
    The formulation factors relevant to developing immediate and controlled release dosage forms containing poorly soluble drugs dispersed in amorphous systems are poorly understood. While the utility of amorphous solid dispersions is becoming apparent in the pharmaceutical marketplace, literature reports tend to concentrate on the development of solid dispersion particulates, which then must be formulated into a tablet. Amorphous solid dispersions of itraconazole in high molecular weight hydroxypropyl methylcellulose were prepared by KinetiSol® Dispersing and tablets were formulated to immediately disintegrate or control the release of itraconazole. Read More

    Self-Assembling Raloxifene Loaded Mixed Micelles: Formulation Optimization, In Vitro Cytotoxicity and In Vivo Pharmacokinetics.
    AAPS PharmSciTech 2017 Nov 27. Epub 2017 Nov 27.
    Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Pune, Maharashtra, 411038, India.
    Raloxifene (RLX) has been strongly recommended for postmenopausal women at high risk of invasive breast cancer and for prevention of osteoporosis. However, low aqueous solubility and reduced bioavailability hinder its clinical application. The objective of this study was to explore the potential of RLX loaded mixed micelles (RLX-MM) using Pluronic F68 and Gelucire 44/14 for enhanced bioavailability and improved anticancer activity on human breast cancer cell line (MCF-7). Read More

    Coenzyme Q10-Loaded Fish Oil-Based Bigel System: Probing the Delivery Across Porcine Skin and Possible Interaction with Fish Oil Fatty Acids.
    AAPS PharmSciTech 2017 Nov 27. Epub 2017 Nov 27.
    School of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Ave, Cardiff, CF10 3NB, UK.
    Coenzyme Q10 (CoQ10) is a vitamin-like oil-soluble molecule that has anti-oxidant and anti-ageing effects. To determine the most optimal CoQ10 delivery vehicle, CoQ10 was solubilised in both water and fish oil, and formulated into hydrogel, oleogel and bigel. Permeability of CoQ10 from each formulation across porcine ear skin was then evaluated. Read More

    Enhancement of Galantamine HBr Skin Permeation Using Sonophoresis and Limonene-Containing PEGylated Liposomes.
    AAPS PharmSciTech 2017 Nov 22. Epub 2017 Nov 22.
    Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, Saitama, 350-0295, Japan.
    This study aimed to investigate the effect of low-frequency sonophoresis (SN) and limonene-containing PEGylated liposomes (PL) on the transdermal delivery of galantamine HBr (GLT). To evaluate the skin penetration mechanism, confocal laser scanning microscopy (CLSM), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were employed. The application of SN led to more GLT penetration into and through the skin than GLT solution alone. Read More

    Fullerenol-Based Intracellular Delivery of Methotrexate: A Water-Soluble Nanoconjugate for Enhanced Cytotoxicity and Improved Pharmacokinetics.
    AAPS PharmSciTech 2017 Nov 20. Epub 2017 Nov 20.
    Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist., Ajmer, Rajasthan, 305817, India.
    Derivatization of fullerenes to polyhydroxylated fullerenes, i.e., fullerenols (FLU), dramatically decreases their toxicity and has been reported to enhance the solubility as well as cellular permeability. Read More

    Fluidized Bed Hot-Melt Granulation as a Tool to Improve Curcuminoid Solubility.
    AAPS PharmSciTech 2017 Nov 16. Epub 2017 Nov 16.
    Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Instituto Nacional de Ciência e Tecnologia-INCT-Nanotecnologia Farmacêutica, Universidade de São Paulo, Via do Café s/n, Campus USP, Ribeirão Preto, SP, 14040-903, Brazil.
    Curcumin is the main bioactive component of Curcuma longa L. and has recently aroused growing interest from the scientific community. Unfortunately, the medicinal properties attributed to curcuminoids are impaired by their low oral bioavailability or low solubility in aqueous solutions. Read More

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