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Pharmaceutical Development and Technology

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https://www.readbyqxmd.com/read/29799300/controlled-delivery-of-the-antiprotozoal-agent-tinidazole-from-intravaginal-polymer-matrices-for-treatment-of-the-sexually-transmitted-infection-trichomoniasis
#1
Hevanshi Vidhushika Fernando, Li Li Chan, Nhung Dang, Diviya Santhanes, Hasini Banneheke, Sivalingam Nalliah, Allan G A Coombes
Microporous polymeric matrices prepared from poly(ɛ-caprolactone) [PCL] were evaluated for controlled vaginal delivery of the antiprotozoal agent (tinidazole) in the treatment of the sexually transmitted infection, trichomoniasis. The matrices were produced by rapidly cooling co-solutions of PCL and tinidazole in acetone to -80 °C to induce crystallisation and hardening of the polymer. Tinidazole incorporation in the matrices increased from 1.4 to 3.9% (w/w), when the drug concentration in the starting PCL solution was raised from 10 to 20% (w/w), giving rise to drug loading efficiencies up to 20%...
July 4, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29799305/dexamethasone-loaded-multi-layer-poly-l-lactic-acid-pluronic-p123-composite-electrospun-nanofiber-scaffolds-for-bone-tissue-engineering-and-drug-delivery
#2
Gebremariam Birhanu, Shima Tanha, Hamid Akbari Javar, Ehsan Seyedjafari, Ali Zandi-Karimi, Banafsheh Kiani Dehkordi
In tissue engineering, it is common to mix drugs that can control proliferation and differentiation of cells into polymeric solutions as part of composite to get bioactive scaffolds. However, direct incorporation of drugs might potentially result in undesired burst release. To overcome this problem, here we developed electrospun multilayer drug loaded poly-l-lactic acid/pluronic P123 (PLLA-P123) composite scaffolds. The drug was loaded into the middle layer. The surface, the mechanical and physiochemical properties of the scaffolds were evaluated...
June 29, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29938558/characterisation-of-fused-deposition-modeling-3d-printers-for-pharmaceutical-and-medical-applications
#3
Tim Feuerbach, Stefanie Kock, Markus Thommes
Fused Deposition Modeling (FDM) is a promising 3D printing technique for the fabrication of personalized drug dosage forms and patient-specific implants. However, there are no market products produced by FDM available at this time. One of the reasons is the lack of a consistent and harmonized approval procedure. In this study, three FDM printers have been characterised with respect to printing parameters relevant for pharmaceutical and medical applications, namely the positioning, hot-end temperature, material residence time, printing velocity and volumetric material flow...
June 25, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29938555/specificity-of-process-analytical-tools-in-the-monitoring-of-multicomponent-pharmaceutical-powders
#4
Pedro Durão, Clémence Fauteux-Lefebvre, Jean-Maxime Guay, Jean-Sébastien Simard, Nicolas Abatzoglou, Ryan Gosselin
The application of Process Analytical Technologies in pharmaceutical manufacturing has been the subject of many studies. Active pharmaceutical ingredient monitoring in real time throughout the manufacturing process is commonly the target of many such implementations. The tools in place must be sensitive to, and selective of, the parameter(s) to be monitored, i.e., in the case of component quantification, they must respond to the component in question and be robust against all others. In the present study, 4 different ingredients (riboflavin, ferrous fumarate, ginseng and ascorbic acid) in a multi-component blend were monitored by 3 different tools (near infrared spectroscopy, laser-induced fluorescence, and red-green-blue camera) using a full factorial design...
June 25, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29781745/using-dextran-of-different-molecular-weights-to-achieve-faster-freeze-drying-and-improved-storage-stability-of-lactate-dehydrogenase
#5
Bjarke Strøm Larsen, Jeppe Skytte, Anna J Svagan, Helena Meng-Lund, Holger Grohganz, Korbinian Löbmann
Freeze-drying of protein formulations is frequently used to maintain protein activity during storage. The freeze-drying process usually requires long primary drying times because the highest acceptable drying temperature to obtain acceptable products is dependent on the glass transition temperature of the maximally freeze-concentrated solution (Tg '). On the other hand, retaining protein activity during storage is related to the glass transition temperature (Tg ) of the final freeze-dried product. In this study, dextrans with different molecular weight (1 and 40 kDa) and mixtures thereof at the ratio 3:1, 1:1, and 1:3 (w/w) were used as cryo-/lyoprotectant and their impact on the stability of the model protein lactate dehydrogenase (LDH) was investigated at elevated temperatures (40 °C and 60 °C)...
June 20, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29781756/development-and-in-vivo-evaluation-of-chitosan-nanoparticles-for-the-oral-delivery-of-albumin
#6
Dalia Nashaat, Mahmoud Elsabahy, Tahra El-Sherif, Mostafa A Hamad, Gamal A El-Gindy, Ehsan H Ibrahim
Albumin is used as a plasma expander in critically ill patients and for several other clinical applications mainly via intravenous infusion. Oral administration of albumin can improve patient compliance although limited oral bioavailability of proteins is still a major challenge. Although nanomaterials have been extensively utilized for improving oral delivery of proteins, albumin has been utilized only as either a model drug or as a carrier for drug delivery. In the current study, for the first time, chitosan nanoparticles have been developed and extensively optimized to improve oral bioavailability of albumin as a therapeutic protein...
June 18, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29897843/design-characterization-and-evaluation-of-aceclofenac-loaded-eudragit-rs-100-nanoparticulate-system-for-ocular-delivery
#7
Rajesh Katara, Sameer Sachdeva, Dipak K Majumdar
The aim of the present study was to develop and evaluate positively charged nanoparticles of aceclofenac for ocular delivery. The nanoparticles were prepared by nanoprecipitation method using Eudragit RS 100. The optimized nanoparticles were found to have narrow particle size range (238.9± 8 nm) with nearly spherical shape, positive zeta potential (40.3 ± 3.8). Higher entrapment efficiency of aceclofenac (94.53±1.0%) with prolonged in vitro drug release profiles was also observed. Powder X-ray diffraction and differential scanning calorimetry studies indicated decrease in crystallinity of drug within the nanoparticulate polymeric matrix...
June 13, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29688120/conjugates-of-tat-and-folate-with-dox-loaded-chitosan-micelles-offer-effective-intracellular-delivery-ability
#8
Shengyu Zhang, Yanjun Liu, Ye Gan, Nanqing Qiu, Yueqing Gu, Hongyan Zhu
The key for better antitumor efficacy is to improve the specificity of antitumor drugs for tumor cells and diminish their cytotoxicity to normal tissues. Targeted nanoparticles as antitumor drug delivery system can resolve this problem. In this study, we prepared folate and TAT (arginine-rich cell-penetrating peptide) modified N-PEG-N'-octyl-chitosan to form the folate/TAT-PEG-OC micelles. Then, the molecular structure, morphology, size distribution and bio-safety of the micelles were characterized. In order to investigate the drug-loading capacity of folate/TAT-PEG-OC micelles, doxorubicin (DOX) was used as model drug to prepare DOX-loaded chitosan micelles...
June 13, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29888992/advances-in-rectal-drug-delivery-systems
#9
Trusha J Purohit, Sara M Hanning, Zimei Wu
Drug delivery via the rectum is a useful alternative route of administration to the oral route for patients who cannot swallow. Traditional rectal dosage forms have been traditionally used for localised treatments including delivery of laxatives, treatment of haemorrhoids and for delivery of antipyretics. However, the recent trend is showing an increased incline for development of novel rectal delivery systems to deliver drug directly into the systemic circulation by taking advantage of porto-systemic shunting...
June 11, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29873575/evaluation-of-paromomycin-sulphate-permeation-using-ex-vivo-human-skin-model
#10
Enam A Khalil, Mahmoud Y Alkawareek, Ghadeer Othman, Bayan Tbakhi, Amal G Al-Bakri
Ex-vivo evaluation of drug release and skin permeation from topical formulations of antileishmanial drug paromomycin sulphate was carried out using intact full thickness human skin. Potency-based microbiological assay was used for the analysis of paromomycin concentrations. A total percentage drug recovery of 86±26% was obtained. Incubation periods of 1 and 3 hours resulted in percentage drug permeation into deep skin layers ranging from 1.3±0.04% to 5.3±2.0% with paraffin-based ointment and from 1.6±0...
June 6, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29863957/incorporation-of-rosuvastatin-loaded-chitosan-chondroitin-sulfate-nanoparticles-into-a-thermosensitive-hydrogel-for-bone-tissue-engineering-preparation-characterization-and-cellular-behavior
#11
Mahboubeh Rezazadeh, Maryam Parandeh, Vajihe Akbari, Zahra Ebrahimi, Azade Taheri
Rosuvastatin (RSV) has been shown to have significant impact on the simulation of bone regeneration after local injection. The current study aimed to develop a localized controlled delivery system from RSV by incorporating RSV-loaded chitosan/chondroitin sulfate (CTS/CS) nanoparticles into thermosensitive Pluronic F127/hyaluronic acid (PF127/HA) hydrogel. RSV-loaded CTS/CS nanoparticles were prepared by ionic gelation and the impact of various formulation variables was assessed using the Box-Behnken design...
June 4, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29757067/a-comparative-study-of-the-influence-of-alpha-lactose-monohydrate-particle-morphology-on-granule-and-tablet-properties-after-roll-compaction-dry-granulation
#12
Simon Grote, Peter Kleinebudde
The influence of particle morphology and size of alpha-lactose monohydrate on dry granules and tablets was studied. Four different morphologies were investigated: Two grades of primary crystals, which differed in their particle size and structure (compact crystals vs. agglomerates). The materials were roll compacted at different specific compaction forces and changes in the particle size distribution and the specific surface area were measured. Afterwards, two fractions of granules were pressed to tablets and the tensile strength was compared to that from tablets compressed from the raw materials...
May 29, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29723110/polyamidoamine-pamam-dendrimers-as-potential-release-modulators-and-oral-bioavailability-enhancers-of-vardenafil-hydrochloride
#13
Mai Ahmed Tawfik, Mina Ibrahim Tadros, Magdy Ibrahim Mohamed
Vardenafil hydrochloride (VAR) is an erectile dysfunction treating drug. VAR has a short elimination half-life (4-5 h) and suffers low oral bioavailability (15%). This work aimed to explore the dual potential of VAR-dendrimer complexes as drug release modulators and oral bioavailability enhancers. VAR-dendrimer complexes were prepared by solvent evaporation technique using four dendrimer generations (G4.5, G5, G5.5 and G6) at three concentrations (190 nM, 380 nM and 950 nM). The systems were evaluated for intermolecular interactions, particle size, zeta potential, drug entrapment efficiency percentages (EE%) and drug released percentages after 2 h (Q2h ) and 24 h (Q24h )...
May 21, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29723078/evaluation-of-the-losartan-solubility-in-the-biowaiver-context-by-shake-flask-method-and-intrinsic-dissolution
#14
Janine Braga de Souza, Jacqueline de Souza, Lara Maria Lopes de Castro, Melissa Fabíola Siqueira, Ranylson Marcello Leal Savedra, Neila Márcia Silva-Barcellos
This study aimed at evaluating the shake-flask use as a universal method to evaluate drug solubility in a biowaiver context as proposed by FDA, EMA and ANVISA. The solubility of losartan was determined in three buffers using the shake-flask method, intrinsic dissolution (ID) and Quantum Chemistry. Moreover, the evaluation of a losartan dissolution profile from coated tablets was conducted. The losartan low solubility in pH 1.2 and high solubility in pH 6.8 were observed using the shake-flask method. However, the solubility results using ID demonstrated its high solubility in pH 1...
May 21, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29741465/preparation-of-biocompatible-copolymeric-micelles-as-a-carrier-of-atorvastatin-and-rosuvastatin-for-potential-anticancer-activity-study
#15
Manjili Hamidreza Kheiri, Niusha Alimohammadi, Hossein Danafar
Statins are widely used for the treatment of hypercholesterolemia. However, their inhibitory action on HMG-CoA reductase also results in the depletion of intermediate biosynthetic products, which importantly contribute to cell proliferation. The aim of the present study was to compare the effects of the individual commercially available statins on investigational breast cancer. Thus, in this study, biodegradable polymeric micelles as carrier of statins were prepared using biodegradable copolymers (PCL-PEG-PCL)...
May 18, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29688126/effect-of-substitution-of-plasticizer-dibutyl-phthalate-with-dibutyl-sebacate-on-eudragit-%C3%A2-rs30d-drug-release-rate-control
#16
Rakesh Singh Chaudhary, Tejas Patel, Job Richard Kumar, Mohamed Chan
In the current study, the influence of type of plasticizer used with Eudragit® RS 30D on the drug release was investigated in solid dosage form extrusion/spheronization, and film coating. The drug pellets were coated for controlling drug release with Eudragit® RS 30D containing dibutyl phthalate and compared with dibutyl sebacate as an alternative plasticizer. To study the influence of pH of the dissolution medium on the drug release profile, capsules are tested for drug release profile at pH 1.2, 4.4, and 6...
May 8, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29688125/mechanical-activation-of-efavirenz-the-effects-on-the-dissolution-and-inhibitory-behavior
#17
E Cappelletto, C Firrito, M Pizzato, L Rebuffi, P Scardi
A poorly water-soluble drug (Efavirenz) was mechanically activated by ball-milling. The effect of the mechanical activation on the dissolution behavior and bioavailability was investigated revealing possible correlations with the grinding action, in terms of crystallinity, particle size and morphology.With proper selection of the grinding parameters the dissolution kinetics can be controlled, both in terms of dissolution velocity and as amount of dissolved drug. In vitro biological tests show that milling does not impair the ability of Efavirenz to inhibit HIV-1 infection (p value >0...
May 8, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29688101/the-efficiency-of-lipid-nanoparticles-with-an-original-cationic-lipid-as-a-sirna-delivery-system-for-macrophages-and-dendritic-cells
#18
Yasunori Uemura, Tomoyuki Naoi, Yasumasa Kanai, Katsuya Kobayashi
Small interfering of RNA (siRNA) technology has the potential to be a next-generation therapy. However, naked siRNA does not have high transfection efficiency and is rapidly degraded after systemic injection, so an appropriate drug delivery system (DDS) is required for clinical use. Several potential systems have been assessed, clinically focusing on hepatocyte or cancer tissue using siRNA. However, targeting immune cells using siRNA is still challenging, and a new DDS is required. In this study, we prepared lipid nanoparticles (LNP) composed of original cationic lipid, neutral lipid of DOPE (1,2-dioleoyl-sn-glycero-3-phosphoethanolamine) and PEG2000-DMPE (N-(carbonyl-methoxypolyethyleneglycol 2000)-1,2-dimyristoyl-sn-glycero-3-phosphoethanolamine, sodium salt)...
May 8, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29688119/squalane-based-emulsion-vaccine-delivery-system-composition-with-murabutide-activate-th1-response
#19
Ravi Kantipakala, Bonam Srinivasa Reddy, Vemireddy Sravanthi, Sreekanth Miryala, Halmuthur M Sampath Kumar
Emulsions play an important role in present day subunit vaccine delivery. Squalane based emulsion was formulated using surfactants viz., Pluronic F68, Span 85 along with Murabutide (MB) as immunepotentiator. Particle size and zetapotential of the final optimized emulsion was found to be 134 nm and -13 mV respectively. The in-vitro cellular uptake studies performed using fluorescein isothiocyanate (FITC)-labeled ovalbumin (OVA) clearly revealed the rapid uptake of antigen in presence of emulsion. The in-vivo subcutaneous studies involving measurement of OVA specific IgG antibody titers, Th1/Th2 cytokines were performed and a marked up regulation in IL-2, IL-12, and IFN-γ cytokines indicate Th1 immune response...
April 24, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29785887/quality-by-design-process-analytical-technology-gmp-and-regulatory-affairs
#20
Metin Çelik
No abstract text is available yet for this article.
July 2018: Pharmaceutical Development and Technology
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