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Drug Development and Industrial Pharmacy

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https://read.qxmd.com/read/30986085/design-and-development-of-a-self-microemulsifying-drug-delivery-system-of-olmesartan-medoxomil-for-enhanced-bioavailability
#1
Yelda Komesli, Ali Burak Ozkaya, Bekir Ugur Ergur, Levent Kirilmaz, Ercument Karasulu
Olmesartan Medoxomil (OM) is a hydrophobic antihypertensive drug with low bioavailability (26%) and is known to have adverse effects such as celiac disease and enteropathy. The purpose of this study was to develop SMEDDS to increase bioavailability and decrease potential side effects of OM. Hydrophilic lipophilic balance was calculated by testing solubility of OM in different oils, surfactants and cosurfactants to obtain the most suitable combination of SMEDDS. Pseudoternary phase diagram was used to select the better oil/water formulation of SMEDDS...
April 15, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30983428/central-composite-rotatable-design-for-optimization-of-budesonide-loaded-cross-linked-chitosan-dextran-sulfate-nanodispersion-characterization-in-vitro-diffusion-and-aerodynamic-study
#2
Divyanka S Bodas, Pradum P Ige
Budesonide is BCS class II drug had low water solubility (0.045 mg/mL) and low oral bioavailability (6-8%) due to high first pass effect. It is aimed to prepare cross linked chitosan-dextran sulfate nanoparticles and/or nanodispersion. Nebulizable cross-linked nanodispersion were prepared by the solvent evaporation technique and characterized through XRPD, FTIR, mean particle size (MPS), polydispersity index (PDI), zeta potential (ZP), drug loading, entrapment efficiency, SEM, % production yield, in vitro diffusion, aerodynamic and stability study...
April 13, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30950303/nanoscaled-pearl-powder-accelerates-wound-repair-and-regeneration-in-vitro-and-in-vivo
#3
Xi Chen, Li-Hua Peng, Seng-Sing Chee, Ying-Hui Shan, Wen-Quan Liang, Jian-Qing Gao
Pearl powder has been used to treat many diseases like palpitations, insomnia, and epilepsy for thousands of years in Chinese medicine. It has demonstrated antioxidant, antiaging, antiradiative, and tonic activities. Pearl powder contains multiple active proteins, which are nutritious for skin cells and might be advantageous for wound repair and regeneration. However, its healing effect in vivo was not reported yet. This study aims to investigate the effects and the underlying mechanism of the pearl powders with different particle sizes in wound treatment...
April 5, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30939950/the-preparation-characterization-of-lupeol-pegylated-liposome-and-its-functional-evaluation-in-vitro-as-well-as-pharmacokinetics-in-rats
#4
Jun Zhang, Huali Liang, Hui Yao, Zhenpeng Qiu, Xinyan Chen, Xixi Hu, Junjie Hu, Guohua Zheng
OBJECTIVE: The objective of this study was to enhance the solubility and bioavailability of Lupeol. METHODS: Utilizing a thin-film dispersion method, we prepared Lupeol-loaded PEGylated liposomes and Lupeol-loaded liposomes, which was characterized by SEM, mean diameter, PDI, zeta potential and entrapment efficiency(EE). The EE, in vitro release and stability of Lupeol-loaded PEGylated liposomes, were detected by HPLC. In addition to the safety evaluation, the evaluation was carried out on HepG2 cells in vitro; the pharmacokinetics were carried out after i...
April 3, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30935249/solubilization-and-determination-of-solution-thermodynamic-properties-of-itraconazole-in-different-solvents-at-different-temperatures
#5
Sachin K Jagdale, Rajesh B Nawale
The solubility of itraconazole (ITRA) in thirteen pure solvents including water, dimethyl sulphoxide, acetonitrile, methanol, 1,4-butanediol, ethanol, isopropyl alcohol, n-butanol, octanol, ethyl acetate, toluene, benzene, 1,4-dioxane were estimated at the temperatures ranging from 293.15 K to 318.15 K under atmospheric pressure (0.1 MPa). The results reflected that the solubility of ITRA was a function of temperature and was increased with rise in temperature in each solvent. Moreover, the solubility in polar solvents was less and found to be increased in non-polar solvents...
April 2, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30932720/design-and-development-of-bioinspired-calcium-phosphate-nanoparticles-of-mtx-pharmacodynamic-and-pharmacokinetic-evaluation
#6
Shweta Pandey, Asiya Mahtab, Vijay Kumar, Farhan Jalees Ahmad, Anita Kamra Verma, Sushama Talegaonkar
The aim of this investigation is the management of rheumatoid arthritis (RA) by developing methotrexate loaded calcium phosphate nanoparticles (MTX-CAP-NP) and to evaluate pharmacokinetic and pharmacodynamic behaviour in adjuvant induced arthritis model. The nanoparticles were synthesized by wet precipitation method and optimized by Box-Behnken experimental design. MTX-CAP-NPs were characterized by TEM, FTIR, DSC and XRD studies. The particle size, zeta potential and entrapment efficiency of the optimized nanoparticles were found to be 204...
April 1, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30929537/development-and-validation-of-a-versatile-hplc-dad-method-for-simultaneous-determination-of-the-antiviral-drugs-daclatasvir-ledipasvir-sofosbuvir-and-ribavirin-in-presence-of-seven-potential-impurities-application-to-assay-of-dosage-forms-and-dissolution-studies
#7
Mostafa M Baker, Sherif F Hammad, Tarek S Belal
This study describes a simple, sensitive, specific and generic HPLC-DAD method for simultaneous determination of four drugs prescribed for treatment of Hepatitis C Virus (HCV) infection. Investigated drugs include daclatasvir (DAC), ledipasvir (LED), sofosbuvir (SOF) and ribavirin (RIB). Successful separation was accomplished using Thermohypersil BDS-C8 column (4.6 × 250 mm, 5 µm) with gradient elution of the mobile phase consisted of mixed phosphate buffer pH 7.5 and methanol. Gradient elution started with 25% methanol, ramped up linearly to 80% in 15 min then kept constant till the end of the run...
April 1, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30922126/formulation-and-optimization-of-intranasal-nanolipid-carriers-of-pioglitazone-for-the-repurposing-in-alzheimer-s-disease-using-box-behnken-design
#8
Gifty M Jojo, Gowthamarajan Kuppusamy, Anindita De, V V S Narayan Reddy Karri
Growing evidence suggest that Alzheimer's disease (AD), the most common cause of dementia among the elderly is a metabolic disorder associated with impaired brain insulin signaling. Hence, the diabetic drug can be a therapeutic option for the management AD. The researches in this area are ongoing and Pioglitazone (PIO) is one of the most investigated diabetic drug in AD. Eventhough PIO treatment was found to improve AD significantly in the preclinical models, the poor blood-brain barrier (BBB) permeability and serious peripheral side effects limited its success in the clinical trials...
March 28, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30922119/synthesis-and-characterization-of-amphiphilic-star-shaped-copolymers-based-on-%C3%AE-cyclodextrin-for-micelles-drug-delivery
#9
Jieqiong Lv, Runcheng Liang, Zihua Xia, Yong Li, Zhufen Lv, Dongzhi Hou, Liping Yu, Gang Chen, Yi Liu, Fan Yang
PURPOSE: A series of β-CD amphiphilic star-shaped copolymers with exceptional characteristics were synthesized and their potential as carriers for micelles drug delivery was investigated. METHODS: A series of amphiphilic copolymers based on β-CD were synthesized by introducing poly (acrylic acid)-co-poly(methyl methacrylate)-poly (vinyl pyrrolidone) or poly (acrylic acid)-co-poly(methyl methacrylate)-co-poly(monoacylated-β-CD)-poly (vinyl pyrrolidone) blocks to the primary hydroxyl group positions of β-CD...
March 28, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30919700/preparation-and-evaluation-of-optimized-zolmitriptan-niosomal-emulgel
#10
Magdy Ibrahim Mohamed, Aly Ahmed Abdelbary, Soha Mohamed Kandil, Tamer Mohamed Mahmoud
OBJECTIVE: Novel niosomal formulation may be successfully applied to treat a systemic disease such as migraine through transdermal drug delivery system (TDDS), moreover, the treatment of tropical diseases such as mycotic infections by targeting and localizing the drug to the stratum corneum. The current study aims to formulate zolmitriptan (Zt) in niosomal vesicles to potentiate its transdermal effect. SIGNIFICANCE: The development of a promising niosomal formulation will push the scaling up of pharmaceutical industry in this field...
March 28, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30913925/mannose-functionalized-plain-and-endosomolytic-nanocomposite-s-based-approach-for-the-induction-of-effective-antitumor-immune-response-in-c57bl-6-mice-melanoma-model
#11
Rajeev Sharma, S P Vyas
The goal of present study to assess the antigen specific immunopotentiation effect of mannose functionalized endosomolytic and conventional nanocomposite(s) based combination approach using C57BL/6 mice melanoma model. Endosomolytic and conventional nanocomposite(s) were prepared by double emulsification method. The optimized formulation was extensively characterized for average particle size, zeta potential and PDI of nanocomposite(s) which were measured in range of ≈200 nm, 0.111 ± 0.024, -23.4 ± 2...
March 26, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30913921/green-isolation-and-physical-modification-of-pineapple-stem-waste-starch-as-pharmaceutical-excipient
#12
Annisa Rahma, Melissa Adriani, Puji Rahayu, Raymond R Tjandrawinata, Heni Rachmawati
The waste of inedible parts of pineapple, particularly in tropical countries, contributes to environmental burden. This study aimed to utilize pineapple stem waste as a source of starch-based pharmaceutical excipient. The starch was isolated from pineapple stem waste using a simple process without applying harsh chemicals. The isolated starch (PSS) was then physically modified through gelatinization and spray drying to improve its physical properties. Starch characteristics were identified by FTIR, TGA, and XRD analysis...
March 26, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30912678/preparation-characterization-and-ex-vivo-in-vivo-assessment-of-candesartan-cilexetil-nanocrystals-via-solid-dispersion-technique-using-an-alkaline-esterase-activator-carrier
#13
Ahmed M Amer, Ahmed N Allam, Ossama Y Abdallah
The objective of this study was to improve candesartan cilexetil (CC) efficacy by formulating nanocrystals via solid dispersion (SD) technique using tromethamine (Tris). SDs was prepared by solvent evaporation at different drug carrier ratios, evaluated for particle size, vitro dissolution studies, TEM, FT-IR and X-ray powder diffraction. Ex vivo, In vivo pharmacokinetic parameters were conducted on selected formulae compared to drug suspension and marketed product. Size analysis demonstrated formation of particles in the nano range lower than 300 nm...
March 26, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30909753/preparation-and-in-vitro-in-vivo-evaluation-of-azilsartan-osmotic-pump-tablets-based-on-the-preformulation-investigation
#14
Nini Li, Ling Fan, Biao Wu, Genlai Dai, Chengjun Jiang, Yan Guo, Dianlei Wang
The objective of this study was to design and evaluate azilsartan osmotic pump tablets. Preformulation properties of azilsartan were investigated for formulation design. Azilsartan osmotic pump tablets were prepared by incorporation of drug in the core and subsequent coating with cellulose acetate and polyethylene glycol 4000 as semi-permeable membrane, then drilled an orifice at the center of one side. The influence of different cores, compositions of semipermeable membrane and orifice diameter on azilsartan release were evaluated...
March 25, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30905176/multivariate-approaches-for-the-development-of-quality-control-in-situ-fiber-optics-dissolution-methods-for-fixed-dose-combination-tablets
#15
Joseph Medendorp, Ivelisse Colón, Taryn Ryan
The purpose of this research was to develop a fiber optic (FO) dissolution method for quantification of multiple actives in combination pharmaceutical tablets. FO dissolution allows direct API quantification in the vessel, obviating the need for error-prone facets of traditional dissolution methods. However, FO dissolution is potentially challenged by overlapping UV spectra, matrix effects, UV-active excipients, API interactions with excipients and media, and undissolved components attenuating the UV signal...
March 25, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30892088/novel-hypolipidemic-conjugates-of-fatty-acid-and-bile-acid-with-lysine-for-linkage
#16
Xue-Yuan Jin, Chuan-Bao Zhu, Shi-Yong Fan, Jia-Lin Sun, Yu-Cong Shi, Chu-Han Wang, Hui-Fen Wang, Bo-Hua Zhong, Yi-Shan Yao, Wei-Guo Shi
Novel fatty acid-bile acid conjugates (1a-1k) were designed and synthesized by coupling of the fatty acids to the 3-OH of bile acids using lysine for linkage. In the conjugates, the 24-COOH of the bile acids was kept intact to preserve liver-specific recognition. The ability of the newly synthesized conjugates (at 100 mg/kg dosage) to reduce total cholesterol (TC) and triglyceride (TG) levels in mice fed with high-fat diet (HFD) was evaluated. Conjugates of stearic acid with cholic acid and palmitic acid with ursodeoxycholic acid (at dosages of 50, 100, and 200 mg/kg) were further evaluated to determine their ability to reduce aspartate aminotransferase (AST), alanine aminotransferase (ALT), TC, and TG levels in mice fed with HFD...
March 20, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30889990/development-and-evaluation-of-dexibuprofen-formulation-with-fast-onset-and-prolonged-effect
#17
Yoonho Choi, Kyoung Ah Min, Chong-Kook Kim
In the present study, in order to improve the solubility and bioavailability of poorly water-soluble dexibuprofen, a novel dexibuprofen-loaded solid dispersion was developed using the spray-drying technique. The controlled-release dexibuprofen formulation was developed by combining the immediate-release dispersion powder and the sustained-release formula. The solid dispersion composed of dexibuprofen/poloxamer 407/hydroxypropyl methylcellulose (HPMC) 2910 (50 cps)/sodium lauryl sulfate (SLS) (10/1/4/0.1 mg) was selected as the immediate-release formulation due to its increased solubility and dissolution rate...
March 19, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30884977/chitosan-tpp-nanoparticles-stabilized-by-poloxamer-for-controlling-the-release-and-enhancing-the-bioavailability-of-doxazosin-mesylate-in-vitro-and-in-vivo-evaluation
#18
Bader M Aljaeid, Khalid M El-Say, Khaled M Hosny
OBJECTIVE: Control the release and enhance the bioavailability of chitosan-doxazosin mesylate nanoparticles (DM-NPs). SIGNIFICANCE: Improve DM bioavailability for the treatment of benign prostatic hyperplasia and hypertension. METHODS: Plackett-Burman design was utilized to screen the variables affecting the quality of DM-NPs prepared by ionic gelation method. The investigated variables were initial drug load (X1 ), chitosan percentage (X2 ), tripolyphosphate sodium (TPP) percentage (X3 ), poloxamer percentage (X4 ), homogenization speed (X5 ), homogenization time (X6 ) and TPP addition rate (X7 )...
March 18, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30883240/solubility-advantage-of-sulfanilamide-and-sulfacetamide-in-natural-deep-eutectic-systems-experimental-and-theoretical-investigations
#19
Tomasz Jeliński, Maciej Przybyłek, Piotr Cysewski
OBJECTIVE: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. SIGNIFICANCE: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing this problem. Among such strategies, those that are environmentally and economically beneficial are of particular interest...
March 18, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30880488/fabrication-of-solid-lipid-nanoparticles-of-lurasidone-hcl-for-oral-delivery-optimization-in-vitro-characterization-cell-line-studies-and-in-vivo-efficacy-in-schizophrenia
#20
Mitali H Patel, Veenu P Mundada, Krutika K Sawant
OBJECTIVE: The aim of the present investigation was to investigate the efficacy of solid lipid nanoparticles (SLNs) to enhance the absorption and bioavailability of lurasidone hydrochloride (LH) following oral administration. METHODS: The LH loaded SLNs (LH-SLNs) were prepared by high pressure homogenization (HPH) method, optimized using box behnken design and evaluated for particle size (PS), entrapment efficiency (EE), morphology, FTIR, DSC, XRD, in vitro release, ex vivo permeation, transport studies across Caco-2 cell line and in vivo pharmacokinetic and pharmacodynamic studies...
March 17, 2019: Drug Development and Industrial Pharmacy
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