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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/28646247/sucrose-octaacetate-chemical-kinetics-and-shelf-lives-at-various-formulation-phs
#1
Shalini Gaddam, William C Stagner
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. A recently reported SOA stability-indicating method was used to perform SOA chemical kinetic and stability studies. As part of the chemical kinetic study, reaction order, activation energies, extrapolated rate constants, pH-rate profiles at 4 and 25°C, and estimated shelf lives at 4 and 25°C at different buffer pHs are provided...
June 23, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28646246/identification-of-particles-in-raw-materials
#2
Kathryn Lee, Markus Lankers, Oliver Valet
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. Sources of materials can be the environment, process equipment and processing, and packaging...
June 23, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28639178/effective-skin-cancer-treatment-by-topical-co-delivery-of-curcumin-and-stat3-sirna-using-cationic-liposomes
#3
Anup Jose, Suman Labala, Kunal Manoj Ninave, Sudeep Kumar Gade, Venkata Vamsi Krishna Venuganti
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. The cell viability studies in B16F10 mouse melanoma cells have shown that the co-delivery of curcumin and STAT3 siRNA significantly (p < 0...
June 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28639177/feasibility-of-focused-beam-reflectance-measurement-fbrm-for-analysis-of-pharmaceutical-suspensions-in-preclinical-development
#4
Kaushalkumar Dave, Paul E Luner, Cecile Forness, Doris Baker, Corinne Jankovsky, Shirlynn Chen
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. Once experimental conditions were optimized, the homogeneity and sedimentation-redispersion of particles in the suspensions were assessed...
June 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28634790/cellulose-acetate-butyrate-ammonio-methacrylate-copolymer-blends-as-a-novel-coating-in-osmotic-tablets
#5
R Ali, M Walther, R Bodmeier
The objective of this work was the preparation of osmotic tablets using polymer blends of cellulose acetate butyrate (CAB) or ethylcellulose with ammonio methacrylate copolymer (Eudragit® RL). The advantage of these coatings in comparison to the traditionally used cellulose acetate is their solubility in safer organic solvents like ethanol. Polymer films were characterized with respect to their water uptake, dry mass loss, and mechanical properties. The effect of the polymer blend ratio on drug release and on the rupture force of the coating was investigated...
June 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28631252/synthesis-and-characterization-of-novel-carboxymethyl-assam-bora-rice-starch-for-the-controlled-release-of-cationic-anticancer-drug-based-on-electrostatic-interactions
#6
Sharmistha Mohapatra, Anees Ahmad Siddiqui, Mohammed Anwar, Neha Bhardwaj, Sohail Akhter, Farhan Jalees Ahmad
Carboxymethyl Assam Bora rice starch (CM-ABRS) was chemically synthesized in non-aqueous medium with the optimum degree of substitution (DS) of 1.23, and physicochemically characterized by FT-IR, DSC, XRD, and SEM analysis. Comparative evaluation of CM-ABRS with native starch (ABRS) for powder flow characteristics, swelling index, apparent solubility, rheological properties, textural properties, and mucoadhesive studies were carried out. The aim of the current work was to investigate the potential of CM-ABRS as a novel carrier for the water-soluble chemotherapeutic, doxorubicin hydrochloride (DOX)...
June 19, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28623571/erratum-to-co-spray-drying-with-hpmc-as-a-platform-to-improve-direct-compaction-properties-of-various-tablet-fillers
#7
JinZhi Li, LiJie Zhao, Xiao Lin, Lan Shen, Yi Feng
No abstract text is available yet for this article.
June 16, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28620763/anticancer-efficacy-of-self-nanoemulsifying-drug-delivery-system-of-sunitinib-malate
#8
Saad M Alshahrani, Abdullah S Alshetaili, Ahmed Alalaiwe, Bader B Alsulays, Md Khalid Anwer, Ramadan Al-Shdefat, Faisal Imam, Faiyaz Shakeel
Sunitinib malate (SM) is reported as a weakly soluble drug in water due to its poor dissolution rate and oral bioavailability. Hence, in the current study, various "self-nanoemulsifying drug delivery systems (SNEDDS)" of SM were prepared, characterized and evaluated for the enhancement of its in vitro dissolution rate and anticancer efficacy. On the basis of solubilization potential of SM in various excipients, "Lauroglycol-90 (oil), Triton-X100 (surfactant) and Transcutol-P (cosurfactant)" were selected for the preparation of SM SNEDDS...
June 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28620762/using-raman-spectroscopy-in-studying-the-effect-of-propylene-glycol-oleic-acid-and-their-combination-on-the-rat-skin
#9
Eman Atef, Njoud Altuwaijri
The permeability enhancement effect of oleic acid (OA) and propylene glycol (PG) as well as their (1:1 v/v) combined mixture was studied using rat skin. The percutaneous drug administration is a challenge and an opportunity for drug delivery. To date, there is limited research that illustrates the mechanism of penetration enhancers and their combinations on the skin. This project aims to explore the skin diffusion and penetration enhancement of PG, OA, and a combination of PG-OA (1:1 v/v) on rat skin and to identify the potential synergistic effect of the two enhancers utilizing Raman spectroscopy...
June 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28612189/the-inclusion-of-chitosan-in-poly-%C3%AE%C2%B5-caprolactone-nanoparticles-impact-on-the-delivery-system-characteristics-and-on-the-adsorbed-ovalbumin-secondary-structure
#10
Sandra Jesus, Elizangela H Fragal, Adley F Rubira, Edvani C Muniz, Artur J M Valente, Olga Borges
This report extensively explores the benefits of including chitosan into poly-ε-caprolactone (PCL) nanoparticles (NPs) to obtain an improved protein/antigen delivery system. Blend NPs (PCL/chitosan NPs) showed improved protein adsorption efficacy (84%) in low shear stress and aqueous environment, suggesting that a synergistic effect between PCL hydrophobic nature and the positive charges of chitosan present at the particle surface was responsible for protein interaction. Additionally, thermal analysis suggested the blend NPs were more stable than the isolated polymers and cytotoxicity assays in a primary cell culture revealed chitosan inclusion in PCL NPs reduced the toxicity of the delivery system...
June 13, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28600665/determination-of-degradation-kinetics-and-effect-of-anion-exchange-resin-on-dissolution-of-novel-anticancer-drug-rigosertib-in-acidic-conditions
#11
Hardikkumar H Patel, Manoj Maniar, Chen Ren, Rutesh H Dave
Rigosertib is a novel anticancer drug in clinical development by Onconova therapeutics, Inc. Currently, it is in pivotal phase III clinical trials for myelodysplastic syndrome (MDS) patients. Chemically, it is a sodium salt of weak acid with low solubility in lower pH solutions. In the preliminary studies, it was found that rigosertib is unstable in acidic conditions and forms multiple degradation products. In this research, drug degradation kinetics of rigosertib were studied in acidic conditions. Rigosertib follows pseudo-first-order general acid catalysis reaction...
June 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28597364/potential-application-of-nanoemulsions-for-skin-delivery-of-pomegranate-peel-polyphenols
#12
Thaisa Baccarin, Elenara Lemos-Senna
Pomegranate peel and seeds have demonstrated to possess antioxidant compounds with potential application to protect the skin against the ultraviolet radiation damage. However, the photoprotection activity is dependent on the amount of these compounds that reach the viable skin layers. In this paper, we describe the in vitro skin permeation and retention of the major pomegranate peel polyphenols using Franz diffusion cells, after entrapping a ethyl acetate fraction (EAF) from Punica granatum peel extract into nanoemulsions (NEs) prepared with pomegranate seed oil (PSO) or medium chain triglyceride oil (MCT)...
June 8, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28589306/application-of-a-biodegradable-polyesteramide-derived-from-l-alanine-as-novel-excipient-for-controlled-release-matrix-tablets
#13
Ana Dora Bonillo Martínez, Inés Carmen Rodríguez Galán, María Victoria Margarit Bellver
This pre-formulation study assays the capacity of the polyesteramide PADAS, poly (L-alanine-dodecanediol-L-alanine-sebacic), as an insoluble tablet excipient matrix for prolonged drug release. The flow properties of PADAS were suitable for tableting, and the compressibility of tablets containing exclusively PADAS was evaluated by ESEM observation of the microstructure. The tablets were resistant to crushing and non-friable and they did not undergo disintegration (typical features of an inert matrix). Tablets containing 33...
June 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28589305/discriminating-ability-of-abbreviated-impactor-measurement-approach-aim-to-detect-changes-in-mass-median-aerodynamic-diameter-mmad-of-an-albuterol-salbutamol-pmdi-aerosol
#14
J David Christopher, Rajni B Patel, Jolyon P Mitchell, Terrence P Tougas, Adrian P Goodey, Jorge Quiroz, Patrik U Andersson, Svetlana Lyapustina
This article reports on results from a two-lab, multiple impactor experiment evaluating the abbreviated impactor measurement (AIM) concept, conducted by the Cascade Impaction Working Group of the International Pharmaceutical Aerosol Consortium on Regulation and Science (IPAC-RS). The goal of this experiment was to expand understanding of the performance of an AIM-type apparatus based on the Andersen eight-stage non-viable cascade impactor (ACI) for the assessment of inhalation aerosols and sprays, compared with the full-resolution version of that impactor described in the pharmacopeial compendia...
June 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28584900/nanosuspension-based-aloe-vera-gel-of-silver-sulfadiazine-with-improved-wound-healing-activity
#15
Md Abul Barkat, Harshita, Iqbal Ahmad, Raisuddin Ali, Satya Prakash Singh, Faheem Hyder Pottoo, Sarwar Beg, Farhan Jalees Ahmad
The present study focuses on the development and characterization of nanosuspension of a poorly soluble drug, silver sulfadiazine (SSD) incorporated in Aloe vera gel (AV-gel) for improving its therapeutic efficacy. The SSD solution in ammonia was subjected to nanoprecipitation in surfactant solution and particle size was optimized by varying concentration of surfactant. Optimized formulation constituted of 5.5% (w/v) Span 20 and 5.5% (w/v) Tween 80 as a dispersing agent and 0.5% (w/v) Poloxamer 188 as a co-surfactant...
June 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28584899/development-of-aerosol-phospholipid-microparticles-for-the-treatment-of-pulmonary-hypertension
#16
Sarah Brousseau, Zimeng Wang, Sweta K Gupta, Samantha A Meenach
Pulmonary arterial hypertension (PAH) is an incurable cardiovascular disease characterized by high blood pressure in the arteries leading from the heart to the lungs. Over two million people in the USA are diagnosed with PAH annually and the typical survival rate is only 3 years after diagnosis. Current treatments are insufficient because of limited bioavailability, toxicity, and costs associated with approved therapeutics. Aerosol delivery of drugs is an attractive approach to treat respiratory diseases because it increases localized drug concentration while reducing systemic side effects...
June 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28584898/factors-affecting-the-dissolution-of-indomethacin-solid-dispersions
#17
Wei Zhang, Chen-Ning Zhang, Yue He, Ban-Yan Duan, Guang-Yi Yang, Wei-Dong Ma, Yong-Hong Zhang
The aim of this study was to investigate the influence of factors such as carrier type, drug/carrier ratio, binary carriers, and preparation method on the dissolution of an insoluble drug, indomethacin (IM), under supersaturation conditions. Using a solvent evaporation (SE) method, poloxamer 188 and PVP K30 showed better dissolution among the selected carriers. Furthermore, as the ratio of carriers increased (drug/carrier ratio from 1:0.5 to 1:2), the dissolution rate increased especially in almost two times poloxamer 188 solid dispersions (SDs), while the reverse results were observed for PVP K30 SDs...
June 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28577126/nanoencapsulation-improves-scavenging-capacity-and-decreases-cytotoxicity-of-silibinin-and-pomegranate-oil-association
#18
Marila C L Marchiori, Cristina Rigon, Priscila M Copetti, Michele R Sagrillo, Letícia Cruz
Silibinin (SB) and pomegranate oil (PO) present therapeutic potential due to antioxidant activity, but the biological performance of both bioactives is limited by their low aqueous solubility. To overcome this issue, the aim of the present investigation was to develop nanocapsule suspensions with PO as oil core for SB encapsulation, as well as assess their toxicity in vitro and radical scavenging activity. The nanocapsule suspensions were prepared by interfacial deposition of preformed polymer method. SB-loaded PO-based nanocapsules (SBNC) showed an average diameter of 157 ± 3 nm, homogenous size distribution, zeta potential of -14...
June 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28577125/preparation-of-nano-and-microstructures-for-drug-delivery
#19
EDITORIAL
Z Ahmad, M Edirisinghe
No abstract text is available yet for this article.
June 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28560506/biomimetic-dissolution-a-tool-to-predict-amorphous-solid-dispersion-performance
#20
Michael M Puppolo, Justin R Hughey, Traciann Dillon, David Storey, Susan Jansen-Varnum
The presented study describes the development of a membrane permeation non-sink dissolution method that can provide analysis of complete drug speciation and emulate the in vivo performance of poorly water-soluble Biopharmaceutical Classification System class II compounds. The designed membrane permeation methodology permits evaluation of free/dissolved/unbound drug from amorphous solid dispersion formulations with the use of a two-cell apparatus, biorelevant dissolution media, and a biomimetic polymer membrane...
May 30, 2017: AAPS PharmSciTech
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