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Pharmaceutical Development and Technology

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...
May 21, 2018: Pharmaceutical Development and Technology
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 kDa 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 and 60°C)...
May 21, 2018: Pharmaceutical Development and Technology
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 14, 2018: Pharmaceutical Development and Technology
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 9, 2018: Pharmaceutical Development and Technology
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 hours (Q2h ) and 24 hours (Q24h )...
May 3, 2018: Pharmaceutical Development and Technology
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 was observed using the shake-flask method. However, the solubility results using ID demonstrated its high solubility in pH1...
May 3, 2018: Pharmaceutical Development and Technology
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...
April 24, 2018: Pharmaceutical Development and Technology
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...
April 24, 2018: Pharmaceutical Development and Technology
Shengyu Zhang, Yanjun Liu, Ye Gan, Nanqing Qiu, Yueqing Gu, Hongyan Zhu
The key for better anti-tumor efficacy is to improve the specificity of anti-tumor drugs for tumor cells and diminish their cytotoxicity to normal tissues. Targeted nanoparticles as anti-tumor 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...
April 24, 2018: Pharmaceutical Development and Technology
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
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)...
April 24, 2018: Pharmaceutical Development and Technology
Shih-Liang Hsi, Peter Surman, Raida Al-Kassas
A highly sensitive and rapid stability indicating ultra-performance liquid chromatographic (UPLC) method was developed for the quantification and identification of isotretinoin in bulk. Chromatographic separation was developed using a gradient elution in a reversed-phase system at flow rate of 0.5 ml/min with 12 min run time. The mobile phase was a gradient mixture of mobile phase A (contained a 30:70:0.5 mixture solution of methanol/purified water/glacial acetic acid) and mobile phase B (contained a 70:25:4...
April 12, 2018: Pharmaceutical Development and Technology
Sevda Şenel, Tansel Comoglu
No abstract text is available yet for this article.
April 6, 2018: Pharmaceutical Development and Technology
Bayan Alemrayat, Abdelbary Elhissi, Husam M Younes
Letrozole (LTZ), an aromatase inhibitor used for the treatment of hormonally-positive breast cancer in postmenopausal women, has poor water solubility, rapid metabolism, and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been designed and characterized, aimed to control the release, potentially maximize the therapeutic efficiency, and minimize the side effects of the drug. LTZ was incorporated into poly(d,l-lactide) (PDLLA) NPs by employing the emulsion-solvent evaporation technique using a range of drug concentrations...
April 5, 2018: Pharmaceutical Development and Technology
Shahram Emami, Khosro Adibkia, Mohammad Barzegar-Jalali, Mohammadreza Siahi-Shadbad
This study explores the preparation and investigation of dissolution properties of piroxicam cocrystals. Differential scanning calorimetry (DSC) was used to determine the capability of resorcinol (RES), methylparaben (MPB), and vanillin (VAN) to form cocrystals with piroxicam (PRX). Generation of cocrystals was attempted by liquid assisted grinding and slurry methods. Cocrystals were characterized by thermal methods, powder X-ray diffraction, and Fourier-transform infrared spectroscopy. Apparent solubility, intrinsic dissolution rate (IDR), and powder dissolution profile of cocrystals were compared with anhydrous piroxicam, piroxicam monohydrate (PRXMH), and previously reported piroxicam-succinic acid cocrystal...
April 4, 2018: Pharmaceutical Development and Technology
Mariya I Vlasenkova, Ekaterina S Dolinina, Elena V Parfenyuk
Encapsulation of therapeutic proteins into particles from appropriate material can improve both stability and delivery of the drugs, and the obtained particles can serve as a platform for development of their new oral formulations. The main goal of this work was development of sol-gel/emulsion method for preparation of silica microcapsules capable of controlled release of encapsulated protein without loss of its native structure. For this purpose, the reported in literature direct sol-gel/W/O/W emulsion method of protein encapsulation was used with some modifications, because the original method did not allow to prepare silica microcapsules capable for protein release...
March 27, 2018: Pharmaceutical Development and Technology
Samane Bayrami, Zahra Esmaili, SeyedAhmad SeyedAlinaghi, Saeed Reza Jamali Moghadam, Sepide Bayrami, Hamid Akbari Javar, Morteza Rafiee Tehrani, Farid Abedin Dorkoosh
The purpose of this research was the fabrication, statistical optimization, and in vitro characterization of insulin-loaded poly(hydroxybutyrate-co-hydroxyvalerate) (PHBV) nanoparticles (INS-PHBV-NPs). Nanopar-ticles were successfully developed by double emulsification solvent evaporation method. The NPs were characterized for particle size, entrapment efficiency (EE%), and polydispersity index (PDI). The NPs also were characterized by scanning electron microscopy (SEM), Fourier transformed infrared spectroscopy (FTIR), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and circular dichroism (CD)...
March 26, 2018: Pharmaceutical Development and Technology
Rosario Pignatello, Tiziana M G Pecora, Giuseppa G Cutuli, Alfio Catalfo, Guido De Guidi, Barbara Ruozi, Giovanni Tosi, Simona Cianciolo, Teresa Musumeci
Trans-resveratrol (RSV) was microencapsulated in Eudragit® RS100 and RL100 resin blends. Lyophilized microspheres were characterized in the solid state for their micromeritic properties and drug loading. FT-IR, PXRD and DSC analyses suggested that RSV formed an intimate microcrystalline dispersion within the polymer network, also confirmed by SEM analysis. This produced a reduced degradation of RSV after storage at 40°C, compared to the neat drug, and a protection of the drug from UV light-induced trans-cis isomerization (60% intact drug was found after 60 sec irradiation at 350 nm, compared to 37% for the pure drug)...
March 22, 2018: Pharmaceutical Development and Technology
Mohamed Mokhtar, Patrick M Gosselin, Lacasse François-Xavier, Patrice Hildgen
Our work aimed at evaluating the use of Permeability glycoprotein (P-gp) inhibiting nanoparticles (NPs) as a part of a suitable oral solid dosage to improve bioavailability. Famotidine (Pepcid®), a stomach acid production inhibitor, was used as a drug model to test our hypothesis. Famotidine-loaded NPs were prepared by solvent emulsion evaporation using PEG grafted on a polylactide acid (PLA) polymer backbone (PLA-g-PEG), with a 5% molar ratio of PEG vs lactic acid monomer and PEG of either 750 or 2000 Da molecular weight...
March 22, 2018: Pharmaceutical Development and Technology
Kantrol Kumar Sahu, Ravi Shankar Pandey
The present study was undertaken with an aim to investigate the potential of targeting colonic mucosa following oral vaccine delivery to generate prophylactic humoral and mucosal immune response. In present study, response surface methodology (RSM) using the central composite design (CCD) was applied for optimization of process and composition to get uniform, stable reproducible eudragit nanoparticles suitable for targeting to colon. The optimized formulation had the composition of 173 μg HBsAg, 250 mg polymers concentration (4:1 combination of Eudragit S-100 and L-100) and 2% w/v Polyvinyl alcohol (PVA) along with adjuvant Monophosphoryl lipid A (MPLA)...
March 20, 2018: Pharmaceutical Development and Technology
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