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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/28550604/microencapsulation-of-%C3%AE-carotene-based-on-casein-guar-gum-blend-using-zeta-potential-yield-stress-phenomenon-an-approach-to-enhance-photo-stability-and-retention-of-functionality
#1
Deepika Thakur, Ashay Jain, Gargi Ghoshal, U S Shivhare, O P Katare
β-Carotene, abundant majorly in carrot, pink guava yams, spinach, kale, sweet potato, and palm oil, is an important nutrient for human health due to its scavenging action upon reactive free radicals wherever produced in the body. Inclusion of liposoluble β-carotene in foods and food ingredients is a challenging aspect due to its labile nature and low absorption from natural sources. This fact has led to the application of encapsulation of β-carotene to improve stability and bioavailability. The present work was aimed to fabricate microcapsules (MCs) of β-carotene oily dispersion using the complex coacervation technique with casein (CA) and guar gum (GG) blend...
May 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28550603/development-of-novel-high-density-gastroretentive-multiparticulate-pulsatile-tablet-of-clopidogrel-bisulfate-using-quality-by-design-approach
#2
Nilesh Desai, Ravindra Purohit
Myocardial infarction, i.e., heart attack, is a fatal condition which is on the increase all over the world. It is reported that a large number of heart attack occur in morning hours which are attributable to platelet aggregation. Chronotherapy at this stage can be crucial. Clopidogrel bisulfate (CLB) is an antiplatelet agent and has become a drug of choice for prevention of heart attack. It is soluble in acidic pH and has a narrow absorption window. So, its long residence time in stomach is desirable. Therefore, a novel high density tablet was developed comprising multiparticulate pellets with pulsatile release necessary to maintain chronotherapy of heart attack...
May 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28540484/simultaneous-comparison-of-two-roller-compaction-techniques-and-two-particle-size-analysis-methods
#3
Tuomas Saarinen, Osmo Antikainen, Jouko Yliruusi
A new dry granulation technique, gas-assisted roller compaction (GARC), was compared with conventional roller compaction (CRC) by manufacturing 34 granulation batches. The process variables studied were roll pressure, roll speed, and sieve size of the conical mill. The main quality attributes measured were granule size and flow characteristics. Within granulations also the real applicability of two particle size analysis techniques, sieve analysis (SA) and fast imaging technique (Flashsizer, FS), was tested...
May 24, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28536796/development-and-evaluation-of-a-family-of-human-face-and-upper-airway-models-for-the-laboratory-testing-of-orally-inhaled-products
#4
Mark W Nagel, Jason A Suggett, Dominic P Coppolo, Jolyon P Mitchell
Many orally inhaled products are supplied with a facemask instead of a mouthpiece, enabling aerosolized medication to be transferred from the inhaler to the lungs when the user lacks the capability to use a mouthpiece. Until recently, laboratory evaluation of an orally inhaled product-facemask was frequently undertaken by removing the facemask, treating the facemask adapter as being equivalent to a mouthpiece. Measurements of delivered drug mass were therefore subject to bias arising from the absence of dead volume, had the facemask been present...
May 23, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28536795/exploration-of-alginates-as-potential-stabilizers-of-nanosuspension
#5
Jian Guan, Yeli Zhang, Qiaoyu Liu, Xin Zhang, Rina Chokshi, Shirui Mao
The objective of this study was to explore the feasibility of using alginate as a potential stabilizer of nanosuspension and elaborate the corresponding stabilization mechanism. Using lovastatin as a Biopharmaceutics Classification System (BCS) II drug model, alginate-stabilized nanosuspension was fabricated by the high-pressure homogenization method. The particle size, zeta potential, short-term stability, and dissolution behavior of the nanosuspension were characterized. Thereafter, the surface morphology, crystallinity, redispersability, and stability of the spray-dried nanosuspension were investigated...
May 23, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28534300/formulation-and-evaluation-of-naringenin-nanosuspensions-for-bioavailability-enhancement
#6
Sonia Gera, Sreekanth Talluri, Nagarjun Rangaraj, Sunitha Sampathi
The clinical potential of naringenin (NRG) is compromised due to its poor aqueous solubility and low oral bioavailability. The study is aimed at addressing these issues by means of naringenin nanosuspensions (NRG-NS) formulated using polyvinylpyrrolidone (PVP K-90) as stabiliser via antisolvent sonoprecipitation method. Optimisation of sonication time, drug concentration and stabilisers was done based on particle size. Characterisation of pure NRG and NRG-NS was carried out by scanning electron microscopy, differential scanning calorimetry (DSC), x-ray powder diffractometry (XRD) and Fourier transform infrared spectroscopy (FTIR)...
May 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28534299/adsorption-onto-mesoporous-silica-using-supercritical-fluid-technology-improves-dissolution-rate-of-carbamazepine-a-poorly-soluble-compound
#7
Aditya V Gandhi, Priyanka Thipsay, Bharat Kirthivasan, Emilio Squillante
The purpose of this research was to design and characterize an immediate-release formulation of carbamazepine (CBZ), a poorly soluble anti-epileptic drug, using a porous silica carrier. Carbon dioxide in its supercritical state (2000 psi, 30-35°C) was used as an anti-solvent to precipitate CBZ onto two particle size variants of silica. Adsorption isotherms were used as a pre-formulation strategy to select optimum ratios of silica and CBZ. The obtained drug-silica formulations were characterized by dissolution studies, differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM)...
May 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28534298/formulation-and-in-vitro-characterization-of-bioactive-mesoporous-silica-with-doxorubicin-and-metronidazole-intended-for-bone-treatment-and-regeneration
#8
Katarzyna Czarnobaj, Magdalena Prokopowicz, Wiesław Sawicki
The purpose of this study was to evaluate the surface mineralization activity and in vitro drug behavior potential of two forms of mesoporous silica: powder and granulate. Ordered mesoporous SiO2 powder was synthesized by surfactant-assisted sol-gel process using tetraethoxysilane as a silica precursor and hexadecyltrimethylammonium bromide as the structure-directing agent. The granulate was prepared using silica powder and ethyl cellulose as a binding agent. Metronidazole (MT)-an anti-inflammatory substance and doxorubicin hydrochloride (ChD)-an anti-cancer drug were chosen as drug models for delivery studies...
May 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28526986/implementation-of-quality-by-design-for-formulation-of-rebamipide-gastro-retentive-tablet
#9
Jung-Myung Ha, Jeong-Woong Seo, Su-Hyeon Kim, Ju-Young Kim, Chun-Woong Park, Yun-Seok Rhee, Eun-Seok Park
The purpose of the present study was to develop a rebamipide (RBM) gastro-retentive (GR) tablet by implementing quality by design (QbD). RBM GR tablets were prepared using a sublimation method. Quality target product profile (QTPP) and critical quality attributes (CQAs) of the RBM GR tablets were defined according to the preliminary studies. Factors affecting the CQAs were prioritized using failure mode and effects analysis (FMEA). Design space and optimum formulation were established through a mixture design...
May 19, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28523633/synthesis-comparison-and-optimization-of-a-humic-acid-quat10-polyelectrolyte-complex-by-complexation-precipitation-versus-extrusion-spheronization
#10
Margaret Siyawamwaya, Yahya E Choonara, Pradeep Kumar, Pierre P D Kondiah, Lisa C du Toit, Viness Pillay
A novel humic acid and polyquaternium-10 polyelectrolyte complex (PEC) was synthesized utilizing two methods and the solubility and permeability of efavirenz (EFV) were established. Complexation-precipitation and extrusion-spheronization were used to synthesize and compare the drug-loaded PECs. The chemical integrity, thermo-mechanical differences, and morphology between the drug-loaded PECs produced by the two methods were assessed by attenuated total reflectance-Fourier transform infrared, differential scanning calorimetry, and SEM...
May 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28523632/co-spray-drying-with-hpmc-as-a-platform-to-improve-direct-compaction-properties-of-various-tablet-fillers
#11
JinZhi Li, LiJie Zhao, Xiao Lin, Lan Shen, Yi Feng
Many commonly used tablet fillers are not suitable for direct compaction process due to insufficient properties, mainly of flowability and compactability. This work therefore aimed to use co-spray drying with HPMC as a platform to improve direct compaction properties of various tablet fillers. Starch, calcium hydrogen phosphate dihydrate (DCPD), and mannitol were chosen as a representative of three types of commonly used fillers (i.e. organic macromolecules, water-insoluble inorganic salts, and water-soluble small molecular carbohydrates), respectively...
May 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28516414/optimized-mucoadhesive-coated-niosomes-as-a-sustained-oral-delivery-system-of-famotidine
#12
Al-Zahraa M Khalifa, Bazigha K Abdul Rasool
The objective of this study is to develop an oral formulation of famotidine niosomes coated with a mucoadhesive polymer, chitosan. Famotidine (FMT) has low oral bioavailability of 40-45% and short half-life between 2.5 to 4 h. Famotidine is classified as class IV in BCS because of its low aqueous solubility (0.1% w/v) and low permeability. Thus, FMT was loaded to the bioadhesive coated niosomes to improve its solubility, enhance its oral bioavailability, and sustain FMT release pattern. Different formulations were prepared by thin-film hydration method and characterized in terms of entrapment efficiency, morphological features, vesicle size, and zeta potential...
May 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28516413/self-emulsification-of-lipidic-drug-delivery-system-in-pure-water-and-in-concentrated-glycerol-solution
#13
Carole Planchette, Annalisa Mercuri, Lorenzo Arcangeli, Manfred Kriechbaum, Peter Laggner
Self-emulsifying drug delivery systems (SEDDS), often intended for oral delivery, are normally explored in biorelevant aqueous media. The high complexity of these multi-component systems leaves the understanding of self-emulsification poor, hindering formulation rationalization. In this work, we aimed to fill this gap by studying the effects of glycerol on the self-emulsification of a ternary component formulation made of 20% w/w Tween 80, 15% w/w Span 80, and 65% w/w Captex 300 Low C6. The behavior of SEDDS in pure water and a binary mixture of water and glycerol (58...
May 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28516412/optimization-of-adhesive-pastes-for-dental-caries-prevention
#14
Patteera Sodata, Apa Juntavee, Niwut Juntavee, Jomjai Peerapattana
Dental caries prevention products available on the market contain only remineralizing agents or antibacterial agents. This study aimed to develop adhesive pastes containing calcium phosphate and α-mangostin for dental caries prevention using the optimization technique. Calcium phosphate was used as a remineralizing agent, and extracted α-mangostin was used as an antibacterial agent. The effect of the independent variables, which were fumed silica, Eudragit(®) EPO, polyethylene glycol, and ethyl alcohol, on the responses was investigated...
May 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28516411/preparation-of-essential-oil-based-microemulsions-for-improving-the-solubility-ph-stability-photostability-and-skin-permeation-of-quercetin
#15
Xia Lv, Tiantian Liu, Huipeng Ma, Yan Tian, Lei Li, Zhen Li, Meng Gao, Jianbin Zhang, Zeyao Tang
Quercetin can bring many benefits to skin based on its various bioactivities. However, the therapeutic effect of quercetin is limited due to the poor water solubility, pH instability, light instability, and skin permeation. The aim of the present work was applying essential oil-based microemulsions to improve the solubility, pH stability, photostability, and skin permeation of quercetin for topical application. Peppermint oil (PO-ME), clove oil (CO-ME), and rosemary oil (RMO-ME) were selected as model essential oils...
May 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28516410/silymarin-loaded-eudragit-nanoparticles-formulation-characterization-and-hepatoprotective-and-toxicity-evaluation
#16
Amira E El-Nahas, Ahmed N Allam, Doaa A Abdelmonsif, Amal H El-Kamel
The objectives of this study were to formulate, characterize silymarin-loaded Eudragit nanoparticles (SNPs) and evaluate their hepatoprotective and cytotoxic effects after oral administration. SNPs were prepared by nanoprecipitation technique and were evaluated for particle size, entrapment efficiency, TEM, solid-state characterization, and in vitro drug release. The hepatoprotective activity was evaluated after oral administration of selected SNPs in carbon tetrachloride-intoxicated rats. Potential in vivo acute cytotoxicity study was also assessed...
May 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28508129/development-and-characterization-of-magnetite-poly-butylcyanoacrylate-nanoparticles-for-magnetic-targeted-delivery-of-cancer-drugs
#17
Margarita López-Viota, Mazen M El-Hammadi, Laura Cabeza, José Prados, Consolación Melguizo, M Adolfina Ruiz Martinez, José L Arias, Ángel V Delgado
A great attention is presently paid to the design of drug delivery vehicles based on surface-modified magnetic nanoparticles. They can, in principle, be directed to a desired target area for releasing their drug payload, a process triggered by pH, temperature, radiation, or even magnetic field. To this, the possibility of forming part of diagnostic tools by enhanced magnetic resonance imaging or that of further treatment by magnetic hyperthermia can be added. Bare particles are rapidly eliminated from the bloodstream by the phagocyte mononuclear system, leading to short biological half-life...
May 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28500485/hydroxyurea-lactose-interaction-study-in-silico-and-in-vitro-evaluation
#18
Kunal B Bachchhao, R R Patil, C R Patil, Dipak D Patil
The Maillard reaction between hydroxyurea (a primary amine-containing drug) and lactose (used as an excipient) was explored. The adduct of these compounds was synthesized by heating hydroxyurea with lactose monohydrate at 60 °C in borate buffer (pH 9.2) for 12 h. Synthesis of the adduct was confirmed using UV-visible spectroscopy and Fourier transform infrared, differential scanning calorimetry, high-pressure liquid chromatography, and liquid chromatography-mass spectrometry studies. An in silico investigation of how the adduct formation affected the interactions of hydroxyurea with its biological target oxyhemoglobin, to which it binds to generate nitric oxide and regulates fetal hemoglobin synthesis, was carried out...
May 12, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28497240/in-vivo-anticancer-efficacy-and-toxicity-studies-of-a-novel-polymer-conjugate-n-acetyl-glucosamine-nag-peg-doxorubicin-for-targeted-cancer-therapy
#19
Smita Pawar, Ketan Mahajan, Pradeep Vavia
A novel polymer-drug conjugate, polyethylene glycol-N-(acetyl)-glucosamine-doxorubicin (PEG-NAG-DOX) was evaluated in this study for its in vivo potential for treatment of tumours demonstrating improved efficacy and reduced toxicity. The proposed polymer-drug conjugate comprised of polyethylene glycol-maleimide (mPEG-MAL, 30000 Da) as a carrier, doxorubicin (DOX) as an anticancer drug and N-acetyl glucosamine (NAG) as a targeting moiety as well as penetration enhancer. Doxorubicin has a potent and promising anticancer activity; however, severe cardiotoxicity limits its application in cancer treatment...
May 11, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28493004/efavirenz-dissolution-enhancement-iv-antisolvent-nanocrystallization-by-sonication-physical-stability-and-dissolution
#20
Gabriela Julianelly Sartori, Livia Deris Prado, Helvécio Vinícius Antunes Rocha
Efavirenz is a fundamental drug in the HIV therapy; however, it has a low bioavailability due to low water solubility. Particle nanonization should enhance its dissolution and therefore its bioavailability. Nanocrystallization is a promising technique for preparing drug nanocrystals. A solution containing efavirenz (EFV) and methanol was added to an aqueous solution of particle stabilizers, under sonication. The adequate polymer stabilizer and its concentration and drug load were evaluated. Particle size and zeta potential of suspensions were measured...
May 10, 2017: AAPS PharmSciTech
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