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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/28078629/effect-of-microneedle-type-on-transdermal-permeation-of-rizatriptan
#1
Chandrateja Uppuluri, Ashraf Sultana Shaik, Tao Han, Atul Nayak, Karthik J Nair, Benjamin R Whiteside, Buchi N Nalluri, Diganta B Das
The present study was aimed to investigate the effect of salient microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation of rizatriptan (RIZ). Studies were carried out using two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 0.9, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PMs) of 0.6 mm length. In the case of the PMs, arrays were applied three times at different places within a 1.77-cm(2) skin area (PM-3) to maintain the MN density closer to 0...
January 11, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28078628/3d-printed-drugs-for-children-are-we-ready-yet
#2
REVIEW
Maren Preis, Heidi Öblom
The first medicine manufactured by three-dimensional (3D) printing was recently approved by the Food and Drug Administration (FDA). The advantages of printing as a manufacturing route enabling more flexibility regarding the dose, and enlarging individual treatment options, have been demonstrated. There is a particular need for flexible drug delivery solutions when it comes to children. Printing as a new pharmaceutical manufacturing technology brings manufacturing closer to the patient and can easily be adjusted to the required dosing scheme, offering more flexibility for treatments...
January 11, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28074422/compacted-multiparticulate-systems-for-colon-specific-delivery-of-ketoprofen
#3
Rodrigo Gomes de Alencar, Aline Carlos de Oliveira, Eliana Martins Lima, Marcílio Sérgio Soares da Cunha-Filho, Stephânia Fleury Taveira, Ricardo Neves Marreto
Pellet-containing tablets for colon-specific drug delivery present higher targeting efficiency and lower costs when compared with monolithic tablets and pellet-filled capsules, respectively. In this study, pellets containing ketoprofen were coated with different acrylic polymers and submitted to compaction. The influence of formulation and process factors on film integrity was then evaluated. Pellets were prepared via extrusion-spheronization and coated using two acrylic polymers (Eudragit® FS 30 D and Opadry® 94 k28327, PMMA and PMA, respectively)...
January 10, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28070851/development-of-a-sustained-antiplaque-and-antimicrobial-chewing-gum-of-a-decapeptide
#4
Abeer M Al-Ghananeem, Kai P Leung, Jabar Faraj, Patrick P DeLuca
The objective of this paper was to design a chewing gum formulation delivery system in situations where typical dental hygiene practice is not practical. Thus, an analog of decapeptide KSL (KSL-W), known to possess antimicrobial and antiplaque activity, was incorporated into a chewing gum formulation containing cetylpyridinium chloride (CPC). The effect of the excipients, xylitol, and peppermint oil on active ingredients in vitro release was also assessed. Gum formulations were prepared with different excipient parameters, including heating xylitol and gum base at 65 or 85°C, using ground and unground xylitol, and the addition of 1...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28070850/zolendronic-acid-conjugated-plga-ultrasmall-nanoparticle-loaded-with-methotrexate-as-a-supercarrier-for-bone-targeted-drug-delivery
#5
Vinay Raichur, Kusum Devi Vemula, Naini Bhadri, Rema Razdan
Drug delivery to deep-seated tissues such as bone has been a major complication till date. This preferential drug delivery is further important in targeting anti-tumour agents to bone metastasis owing to its complexity. The present study involves the formulation of PLGA nanoparticles and conjugation with zolendronic acid-a bisphosphonate which will anchor the nanosystem to bone due to its selective bone affinity. The conjugated nanosystem was characterized for particle size by TEM (average 36 nm) and morphology by AFM depicting surface irregularities due to ZOL conjugation on the surface of nanoparticles...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28070849/investigation-into-the-manufacture-and-properties-of-inhalable-high-dose-dry-powders-produced-by-comilling-api-and-lactose-with-magnesium-stearate
#6
Michael Lau, Paul M Young, Daniela Traini
The aim of the study was to understand the impact of different concentrations of the additive material, magnesium stearate (MGST), and the active pharmaceutical ingredient (API), respectively, on the physicochemical properties and aerosol performance of comilled formulations for high-dose delivery. Initially, blends of API/lactose with different concentrations of MGST (1-7.5% w/w) were prepared and comilled by the jet-mill apparatus. The optimal concentration of MGST in comilled formulations was investigated, specifically for agglomerate structure and strength, particle size, uniformity of content, surface coverage, and aerosol performance...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28070848/intravaginal-delivery-of-polyphenon-60-and-curcumin-nanoemulsion-gel
#7
Atinderpal Kaur, Yashaswee Saxena, Rakhi Bansal, Sonal Gupta, Amit Tyagi, Rakesh Kumar Sharma, Javed Ali, Amulya Kumar Panda, Reema Gabrani, Shweta Dang
Polyphenon 60 (P60) and curcumin (CUR) were loaded in a single nanoemulsion system and their combined antibacterial action was studied against uropathogenic Escherichia coli. To enhance availability at target organs and to inhibit enzymatic degradation in gastro intestinal tract, vaginal route of administration was explored. P60 + CUR nanoemulsion (NE) was formulated by ultra-sonication and optimized using Box-Behnken design. Optimized NE showed Z-average of 211.2 nm, polydispersity index of 0.343, and zeta potential of -32...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28070847/role-of-water-sorption-in-tablet-crushing-strength-disintegration-and-dissolution
#8
M Sacchetti, R Teerakapibal, K Kim, E J Elder
Drugs formulated as tablets are subjected to accelerated stability conditions with the goal of identifying a stable formulation that will exhibit a sufficiently long shelf life. Water sorption at a condition such as 40°C/75% RH can result in significant changes in tablet properties such as a decrease in dissolution rate, the cause of which may be difficult to interpret, given the complex nature of ingredients and their interactions in a tablet. In this research, three drugs, displaying a wide range of physicochemical properties, were formulated with commonly used diluents, disintegrants, and binders, using a design of experiments approach...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28070846/development-of-a-convenient-in-vitro-gel-diffusion-model-for-predicting-the-in-vivo-performance-of-subcutaneous-parenteral-formulations-of-large-and-small-molecules
#9
Dennis H Leung, Yash Kapoor, Candice Alleyne, Erika Walsh, Andrew Leithead, Bahanu Habulihaz, Gino M Salituro, Annette Bak, Timothy Rhodes
Parenteral delivery remains a compelling drug delivery route for both large- and small-molecule drugs and can bypass issues encountered with oral absorption. For injectable drug products, there is a strong patient preference for subcutaneous administration due to its convenience over intravenous infusion. However, in subcutaneous injection, in contrast to intravenous administration, the formulation is in contact with an extracellular matrix environment that behaves more like a gel than a fluid. This can impact the expected performance of a formulation...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28063103/gentamicin-eluting-titanium-dioxide-nanotubes-grown-on-the-ultrafine-grained-titanium
#10
Sima Hashemi Nemati, Afra Hadjizadeh
Titanium (Ti)-based materials is the most appropriate choices for the applications as orthopedic and dental implants. In this regard, ultrafine-grained (UFG) titanium with an enhanced mechanical properties and surface energy has attracted more attention. Titanium dioxide (TiO2) nanotubes grown on the titanium could enhance bone bonding, cellular response and are good reservoirs for loading drugs and antibacterial agents. This article investigates gentamicin loading into and release from the TiO2 nanotubes, grown on the UFG compared to coarse-grained (CG) titanium substrate surfaces...
January 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28050711/torsemide-fast-dissolving-tablets-development-optimization-using-box-bhenken-design-and-response-surface-methodology-in-vitro-characterization-and-pharmacokinetic-assessment
#11
Ahmed A El-Shenawy, Mahmoud M Ahmed, Heba F Mansour, Saleh Abd El Rasoul
The present study planed to develop new fast dissolving tablets (FDTs) of torsemide. Solid dispersions (SDs) of torsemide and sorbitol (3:1) or polyvinylpyrrolidone (PVP) k25 were prepared. The prepared SDs were evaluated for in-vitro dissolution. Fourier transform infrared spectroscopy and differential scanning calorimetry for SDs revealed no drug/excipient interactions and transformation of torsemide to the amorphous form. Torsemide/sorbitol SD was selected for formulation of torsemide FDTs by direct compression method...
January 3, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28039572/formulation-and-optimization-of-multiparticulate-drug-delivery-system-approach-for-high-drug-loading
#12
Neha Shah, Tejal Mehta, Mukesh Gohel
The aim of the present work was to develop and optimize multiparticulate formulation viz. pellets of naproxen by employing QbD and risk assessment approach. Mixture design with extreme vertices was applied to the formulation with high loading of drug (about 90%) and extrusion-spheronization as a process for manufacturing pellets. Independent variables chosen were level of microcrystalline cellulose (MCC)-X 1, polyvinylpyrrolidone K-90 (PVP K-90)-X 2, croscarmellose sodium (CCS)-X 3, and polacrilin potassium (PP)-X 4...
December 30, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28035612/transdermal-adhesive-patches-loaded-with-ketoprofen-evaluated-by-dynamic-detection-of-percutaneous-absorption
#13
Menglin Wang, Longwei Li, Junxia Xie, Yinghua Sun, Guixia Ling, Zhonggui He
Topical delivery has many benefits toward NSAIDs administration, and the best-selling transdermal preparation in 2015 was the NSAID patch MOHRUS®. Herein, we report a ketoprofen adhesive patch (KAP) and evaluate the penetration and absorption compared to MOHRUS®. Microdialysis sampling technique was applied to determine drug penetration in the dermis and subcutaneous tissue. Simultaneously, blood samples were withdrawn over time to obtain the drug absorption in plasma. The ketoprofen concentrations in the dermis, subcutaneous tissue, and plasma were compared with the commercially available patch (MOHRUS®)...
December 29, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28035611/the-in-vitro-vivo-evaluation-of-prepared-gastric-floating-tablets-of-berberine-hydrochloride
#14
Jun Ji, Xin He, Xiao-Lin Yang, Wen-Juan Du, Cheng-Long Cui, Ling Wang, Xue Wang, Chun-Feng Zhang, Chang-Run Guo
Currently available antiulcer drugs suffered from serious side effects which limited their uses and prompted the need for a safe and efficient new antiulcer agent. The objective of this project work was to retain the drug in the stomach for better antiulcer activity and less side effects. Hence, the aim of our present work was to prepare a gastric floating tablet of Berberine hydrochloride (Ber) with suitable in vitro/vivo properties. In this study, different Ber gastric floating tablets were prepared by simple direct compression using various amounts of HPMCK15M and Carbopol 971PNF combined with other tablet excipients...
December 29, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28028795/membrane-loaded-doxorubicin-liposomes-based-on-ion-pairing-technology-with-high-drug-loading-and-ph-responsive-property
#15
Hang Xu, Lu Zhang, Lin Li, Yang Liu, Yanhui Chao, Xiaolin Liu, Zeng Jin, Yinrong Chen, Xing Tang, Haibing He, Qiming Kan, Cuifang Cai
In order to achieve high drug loading and high entrapment efficiency, a doxorubicin-cholesteryl hemisuccinate ion-pair complex (DCHIP) was formed, and the ion-pair complex liposomes (DCHIP-Lip) were prepared based on conventional thin-film dispersion method. Firstly, DCHIP was fabricated and confirmed with FTIR, (1)H-NMR, DSC, and XRD techniques. Afterwards, DCHIP-Lip were prepared and evaluated in terms of particle size, zeta potential, entrapment efficiency, and drug loading content. Finally, the in vitro and in vivo behavior of liposomes was further investigated...
December 27, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28028794/effect-of-liquid-crystalline-systems-containing-antimicrobial-compounds-on-infectious-skin-bacteria
#16
Carla Souza, Evandro Watanabe, Carolina Patrícia Aires, Marilisa Guimarães Lara
This study aimed (i) to prepare liquid crystalline systems (LCS) of glyceryl monooleate (GMO) and water containing antibacterial compounds and (ii) to evaluate their potential as drug delivery systems for topical treatment of bacterial infections. Therefore, LCS containing CPC (cetylpyridinium chloride) (LCS/CPC) and PHMB (poly(hexamethylene biguanide) hydrochloride) (LCS/PHMB) were prepared and the liquid crystalline phases were identified by polarizing light microscopy 24 h and 7 days after preparation...
December 27, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28028793/in-vitro-drug-transfer-due-to-drug-retention-in-human-epidermis-pretreated-with-application-of-marketed-estradiol-transdermal-systems
#17
Yellela S R Krishnaiah, Naresh Pavurala, Yang Yang, Prashanth Manda, Usha Katragadda, Yongsheng Yang, Rakhi Shah, Guodong Fang, Mansoor A Khan
Study objective was to assess skin-to-skin drug transfer potential that may occur due to drug retention in human epidermis (DRE) pretreated with application of estradiol transdermal drug delivery systems (TDDS) and other estradiol transdermal dosage forms (gels and sprays). TDDS (products-A, B, and C) with varying formulation design and composition, and other estradiol transdermal products (gel and spray) were applied to heat separated human epidermis (HSE) and subjected to in vitro drug permeation study. Amounts of DRE were quantified after 24 h...
December 27, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28028792/in-vitro-and-ex-vivo-evaluation-of-novel-curcumin-loaded-excipient-for-buccal-delivery
#18
Flavia Laffleur, Franziska Schmelzle, Ariane Ganner, Stefan Vanicek
This study aimed to develop a mucoadhesive polymeric excipient comprising curcumin for buccal delivery. Curcumin encompasses broad range of benefits such as antioxidant, anti-inflammatory, and chemotherapeutic activity. Hyaluronic acid (HA) as polymeric excipient was modified by immobilization of thiol bearing ligands. L-Cysteine (SH) ethyl ester was covalently attached via amide bond formation between cysteine and the carboxylic moiety of hyaluronic acid. Succeeded synthesis was proved by H-NMR and IR spectra...
December 27, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28004344/preparation-and-characterization-of-copolymer-micelles-for-the-solubilization-and-in-vitro-release-of-luteolin-and-luteoloside
#19
Weixia Qing, Yong Wang, Huan Li, Fanyi Ma, Jinhua Zhu, Xiuhua Liu
Luteolin (LUT) and luteoloside (LUS) belong to flavonoids with high anticancer potential and were loaded into biodegradable diblock copolymer micelles of methoxy polyethylene glycol-polycaprolactone (mPEG5K-PCL10K), methoxy polyethylene glycol-polylactide-co-glycolide (mPEG5K-PLGA10K), and methoxy polyethylene glycol-polylactide (mPEG5K-PDLLA10K) by a self-assembly method, creating water-soluble LUT and LUS copolymer micelles, respectively. The solubilization formulations of the copolymer micelles were optimized with response surface methodology (RSM)...
December 21, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28004343/naproxen-microparticulate-systems-prepared-using-in-situ-crystallisation-and-freeze-drying-techniques
#20
Amanda Solaiman, Adam Keenan Tatari, Amal Ali Elkordy
Poor drug solubility and dissolution rate remain to be one of the major problems facing pharmaceutical scientists, with approximately 40% of drugs in the industry categorised as practically insoluble or poorly water soluble. This in turn can lead to serious delivery challenges and poor bioavailability. The aim of this research was to investigate the effects of the surfactants, poloxamer 407 (P407) and caprol® PGE 860 (CAP), at various concentrations (0.1, 0.5, 1 and 3% w/v) on the enhancement of the dissolution properties of poorly water-soluble drug, naproxen, using in situ micronisation by solvent change method and freeze-drying...
December 21, 2016: AAPS PharmSciTech
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