Pharmacokinetic evaluation of differential drug release formulations of rabeprazole in dogs.
Conclusions: The use of a canine model has enabled the selection of a novel dual-release prototype formulation of rabeprazole for further clinical development. PMID: 31216902 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - June 22, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Pharmacology mechanism of Flos magnoliae and Centipeda minima for treating Allergic Rhinitis based on Pharmacology network.
Authors: Liang Y, Zhang X, Zou J, Shi Y, Wang Y, Tai J, Yang Y, Zhou X, Guo D, Wang J, Cheng J, Yang M Abstract Chinese herbs such as Flos magnoliae (FM) and Centipeda minima (CM) can be effective in treating allergic rhinitis (AR). However, there is little research on the therapeutic mechanism of these two drugs acting on AR at the same time. In order to systematically understand the mechanism of action of two drugs acting on AR at the same time, we searched various databases to obtain 31 components and 289 target proteins of FM, 25 components and 465 target proteins of CM. The interaction networks of FM, CM and A...
Source: Drug Development and Industrial Pharmacy - June 22, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Influence of omega fatty acids on skin permeation of a coenzyme Q10 nanoemulsion cream formulation: characterization, in silico and ex vivo determination.
Conclusion: CoQ10 loaded-linseed oil nanoemulsion cream displayed the highest skin permeation. The highest permeation showed by linseed oil nanoemulsion cream may be due to the presence of omega-3, -6, and -9 fatty acids which might serve as permeation enhancers. This indicated that the edible oil nanoemulsion creams have potential as drug vehicles that enhance CoQ10 delivery across skin. PMID: 31216907 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - June 22, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Pharmacokinetic, toxicokinetic, and bioavailability studies of epigallocatechin-3-gallate loaded solid lipid nanoparticle in rat model.
Authors: Ramesh N, Mandal AKA Abstract Epigallocatechin-3-gallate (EGCG), derived from green tea, is an active phytochemical against many types of cancer, cardiovascular, neurological and inflammatory diseases. However, its pharmaceutical activity is limited due to low bioavailability and chemical instability. To overcome these limitations, we fabricated spherical, EGCG loaded solid lipid nanoparticles (SLN-EGCG) as an oral delivery system. The SLN-EGCG showed a hydrodynamic diameter of 300.2 ± 3.8 nm with the drug encapsulation efficiency of 81 ± 1.4%. Additionally,...
Source: Drug Development and Industrial Pharmacy - June 20, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

A Review on Parenteral Delivery of Peptides and Proteins.
Authors: Jain D, Mahammad S, Singh PP, Kodipyaka R Abstract The recent advances in pharmaceutical industry in the area of drug delivery and development have resulted into wide variety of biomolecules, particularly peptides and proteins, to palliate the treatment for severe diseases. The rampant development of peptides and proteins in industry mandate the understanding of their characteristic nature and developability. Despite their therapeutic potential, peptides and proteins pose complex challenges in drug delivery and require scientist to contemplate to achieve suitable delivery system. As most of the commercial ...
Source: Drug Development and Industrial Pharmacy - June 20, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Deriving Control Parameter Settings from Process Models to Control Capsule Fillers Integrated into Continuous Manufacturing.
In this study, we developed a method to derive the control parameters based on process models in order to obtain optimal control for each filled product. Determined via rapid automated process development [1], this method is an effective and fast way of determining control parameters. The method allowed us to optimize the weight control for three pharmaceutical excipients. By conducting experiments, we verified the feasibility of the proposed method and studied the dynamics of the controlled system. Our work provides important basic data on how a capsule filler can be implemented into continuous manufacturing systems. ...
Source: Drug Development and Industrial Pharmacy - June 20, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Optimization of the process variables of roller compaction, on the basis of granules characteristics (flow, mechanical strength and disintegration behavior): An application of SeDeM-ODT expert system.
Authors: Khan A Abstract Objective of the study was application of SeDeM-ODT expert system for optimization of process variables for roller compaction and for the preparation of granules with better flow, compressibility and disintegration behavior. In the present study, granules were prepared at pre-determined (on the basis of factorial design) process variables and characterized using SeDeM-ODT expert system. Compatibility of ribavirin with excipients (microcrystalline cellulose, tablettose-80, cross carmellose sodium and magnesium stearate) was evaluated by binary mixture approach, using FTIR. According to SeDeM...
Source: Drug Development and Industrial Pharmacy - June 19, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Combined chemo/photothermal therapy based on mesoporous silica-Au core-shell nanoparticles for hepatocellular carcinoma treatment.
Authors: Wang J, Zhang Y, Liu L, Cui Z, Liu X, Wang L, Li Y, Li Q Abstract Chemotherapy has been widely used for treatment to malignant cancer, such as hepatocellular carcinoma (HCC). Chemotherapeutic effect was not often efficient to achieve totally tumor ablation due to the poor cellular uptake and drug resistance. To address these problems, a novel nanoplatform was constructed based on non-toxic Mesoporous Silica Nanoparticles (MSNs) for a combined chemo/photothermal therapy to enhance tumor cell accumulation and promote toxicity of chemotherapeutic drugs. Prepared MSNs were consisted of Au nanoshell for phototh...
Source: Drug Development and Industrial Pharmacy - June 9, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Enhanced oral delivery and anti-gastroesophageal reflux activity of curcumin by binary mixed micelles.
Authors: Sun Y, Li Y, Shen Y, Wang J, Tang J, Zhao Z Abstract The aim of this study was to improve the solubility, oral bioavailability, and anti-gastroesophageal reflux activity of curcumin by preparing two curcumin-loaded, novel, binary mixed micelles (CM-M). The two CM-M were prepared by ethanol thin-film hydration method. One (CM-T) was prepared using D-alpha-tocopheryl polyethylene glycol 1000 succinate and Solutol®HS15, and the other (CM-F) was prepared using Pluronic®F127 and Solutol®HS15. The entrapment efficiency and drug loading of CM-T were 83.61 ± 0.54% and 2.20 &...
Source: Drug Development and Industrial Pharmacy - June 8, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Formulation development and accelerated stability testing of a novel sunscreen cream for ultraviolet radiation protection in high altitude areas.
Authors: Sharma Bora N, Mazumder B, Patowary P, Kishor S, Doma Bhutia Y, Chattopadhyay P, Dwivedi SK Abstract The present study is aimed at the development of a sunscreen cream for use in high altitude areas which have been found to possess superior sun protection factor (SPF) along with remarkable antioxidant activity. The topical formulation is a standard oil-in-water emulsion of a combination of United States Food and Drug Administration (US FDA) approved ultraviolet filters; along with melatonin and pumpkin seed oil. The in-silico optimized formulation was characterized using established methods and the stabili...
Source: Drug Development and Industrial Pharmacy - May 24, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Drug-polymer miscibility, interactions, and precipitation inhibition studies for the development of amorphous solid dispersions for the poorly soluble anticancer drug flutamide.
Authors: Trivino A, Gumireddy A, Meng F, Prasad D, Chauhan H Abstract The major goal of this research was to successfully formulate solid dispersion (SD) of the poorly soluble anticancer drug flutamide (FLT) using various hydrophilic polymers. Furthermore, to get more insight into SD, solid-state studies (miscibility and molecular interaction) were correlated with solution study (precipitation inhibition, dissolution). Hydrophilic polymers like PVP K90, HPMC, Eudragit EPO, and PEG 8000 were used at different drug-to-polymer w/w ratios. Solid-state miscibility studies were carried out using modulated differential sc...
Source: Drug Development and Industrial Pharmacy - May 23, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Pharmaceutical Quantification with Univariate Analysis Using Transmission Raman Spectroscopy.
Authors: Shimamura R, Koide T, Hisada H, Inoue M, Fukami T, Katori N, Goda Y Abstract The purpose of this study was to investigate the quantification performance of transmission Raman spectroscopy with univariate analysis. Model dosage forms containing acetaminophen and an excipient, lactose monohydrate, were prepared. Raman spectra of the tablets were obtained using the modes of transmission, backscattering micro-spectroscopy, and wide area illumination. Calibration curves for quantification of acetaminophen in the tablets were created using peak heights of the Raman spectra. Of the three modes of measurement, the...
Source: Drug Development and Industrial Pharmacy - May 22, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

High Performance Liquid Chromatography Method Applied to Investigate Mechanism, Kinetics, Isotherm and Thermodynamics of Bile Acid Adsorption onto Bile Acid Sequestrants.
Authors: Raina S, Mungantiwar A, Halde S, Pandita N Abstract The purpose of the study was to develop and validate a high performance liquid chromatography method which can be further applied to understand the mechanism, kinetics, isotherm and thermodynamics of bile acid adsorption onto bile acid sequestrants. To investigate these properties a high performance liquid chromatography method was developed using peerless C-8 (150 x 4.6 mm, 5µm) column with a detection wavelength of 200 nm and run time of about 12.5 minutes. Bile salts Glycocholic acid (GC), Glycochenodeoxycholic acid (GCDC) an...
Source: Drug Development and Industrial Pharmacy - May 22, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Harmine loaded Galactosylated Pluronic F68-Gelucire 44/14 mixed micelles for liver targeting.
Authors: Kushwaha JP, Baidya D, Patil S Abstract Harmine (HM), a phytoconstituent has wide range of pharmacological activities including antimicrobial, antifungal, antioxidative and anticancer. HM has shown promising anticancer activity against liver cancer cells. However, poor aqueous solubility, multidrug pump P-gp efflux, extensive in vivo metabolism and rapid elimination due to glucuronidation/sulfation limits clinical utility of HM. In order to overcome the drawbacks of HM, the current work reports preparation of HM loaded galactosylated pluronic F-68 (PF68)-Gelucire® 44/14(GL44) mixed micelles (HM-MM). 32...
Source: Drug Development and Industrial Pharmacy - May 19, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Stability test of novel combined formulated dry powder inhalation system containing antibiotic: Physical characterization and in vitro-in silico lung deposition results.
CONCLUSION: It can be established that after the storage a novel combined formulated DPI contained amorphous drug to have around 2.5 μm mass median aerodynamic diameter and nearly 50% fine particle fraction predicted high lung deposition in silico also. PMID: 31096805 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - May 19, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Nanocarrier based systems for wound healing.
Authors: Bernal-Chávez S, Nava-Arzaluz MG, Quiroz-Segoviano RIY, Ganem-Rondero A Abstract In general, the systems intended for the treatment and recovery of wounds, seek to act as a coating for the damaged area, maintaining an adequate level of humidity, reducing pain, and preventing the invasion and proliferation of microorganisms. Although many of the systems that are currently on the market meet the purposes mentioned above, with the arrival of nanotechnology, it has sought to improve the performance of these coatings. The variety of nano-systems that have been proposed is very extensive, including the us...
Source: Drug Development and Industrial Pharmacy - May 19, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Comparative Lyophilized Platelet-Rich Plasma Wafer and Powder for Wound Healing Enhancement: Formulation, In vitro and In vivo Studies.
Authors: Yassin GE, Dawoud MHS, Wasfi R, Maher A, Fayez AM Abstract Platelet-rich plasma (PRP) accelerates wound healing, as it is an excellent source of growth factors. PRP was separated from whole human blood by centrifugation. PRP powder and wafers were prepared by lyophilization, with the wafers prepared using sodium carboxymethylcellulose (Na CMC). The PRP wafers showed porous structures, as indicated by scanning electron microscopy (SEM) images, and the ability of the wafer to absorb exudates and thus promote wound healing was tested with the hydration capacity test. The platelet count was tested and indicate...
Source: Drug Development and Industrial Pharmacy - May 19, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Design of selegiline loaded Bio-nanosuspension for the management of depression using novel Bio-retardant from Manilkara zapota.
CONCLUSION: The prepared bio-nanosuspension was found to be safe and compatible with the ophthalmic delivery for treatment of depression. PMID: 31084445 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - May 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Formulation and biopharmaceutical evaluation of risperidone loaded chitosan nanoparticles for intranasal delivery.
CONCLUSION: Risperidone loaded chitosan nanoparticles were effective against schizophrenia via intranasal route. PMID: 31094571 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - May 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Pharmacokinetic and pharmacodynamic modeling of gut hormone peptide YY(3-36) after pulmonary delivery.
Authors: Shao J, Chen MJ, Kuehl PJ, Hochhaus G Abstract Peptide YY(3-36) (PYY(3-36)) is an endogenous appetite suppressing peptide. The present research was to perform pharmacokinetic/pharmacodynamic (PK/PD) analysis for predicting the concentration- and response-time profiles of PYY(3-36) after systemic and pulmonary delivery in mice, with the goal of suggesting a potential pulmonary dosing regimen in humans. A PK/PD model was developed to describe PYY(3-36) plasma concentration - and relative food intake rate ratio (as % of control) - time profiles after intraperitoneal and subcutaneous administration, and inhala...
Source: Drug Development and Industrial Pharmacy - May 3, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Carrier-free combination dry powder inhaler formulation of ethionamide and moxifloxacin for treating drug-resistant tuberculosis.
This study aimed to develop a combination dry powder formulation of ethionamide and moxifloxacin HCl as this combination is synergistic against drug-resistant Mycobacterium tuberculosis (Mtb). L-leucine (20% w/w) was added in the formulations to maximize the process yield. Moxifloxacin HCl and/or ethionamide powders with/without L-leucine were produced using a Buchi Mini Spray-dryer. A next generation impactor (NGI) was used to determine the in vitro aerosolization efficiency. The powders were also characterized for other physicochemical properties and cytotoxicity. All the spray-dried powders were within the aerodynamic size range of
Source: Drug Development and Industrial Pharmacy - April 26, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Exploring the influence of particle shape and air velocity on the flowability in the respiratory tract: a computational fluid dynamics approach.
Authors: Ali AM, Abo Dena AS, Yacoub MH, El-Sherbiny IM Abstract Dry powder inhalers (DPIs) are considered a main drug delivery system through pulmonary route. The main objective of this work is to study the flow of differently shaped microparticles in order to find the optimum shape of drug particles that will demonstrate the best flow to the deep lung. The flowability of particles in air or any fluid depends particularly on the drag force which is defined as the resistance of the fluid molecules to the particle flow. One of the most important parameters that affect the drag force is the particles' shape. Computat...
Source: Drug Development and Industrial Pharmacy - April 24, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Solubility measurement, Hansen solubility parameters and solution thermodynamics of gemfibrozil in different pharmaceutically used solvents.
Authors: Kalam MA, Alshehri S, Alshamsan A, Alkholief M, Ali R, Shakeel F Abstract Gemfibrozil (GEM) is cholesterol-lowering agent which is being proposed as poorly water soluble drug (PWSD). Temperature based solubility values of GEM are not yet available in literature or any pharmacopoeia/monograph. Hence, the present studies were carried out to determine the solubility of PWSD GEM (as mole fraction) in various pharmaceutically used solvents such as "water (H2O), methanol (MeOH), ethanol (EtOH), isopropanol (IPA), 1-butanol (1-BuOH), 2-butanol (2-BuOH), ethylene glycol (EG), propylene glycol (PG), polyethyle...
Source: Drug Development and Industrial Pharmacy - April 20, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

UNBS5162 as a novel naphthalimide holds efficacy in human gastric carcinoma cell behaviors mediated by AKT/ERK signaling pathway.
CONCLUSION: UNBS5162 could restrain gastric carcinoma cell proliferation, invasion and migration, which was maybe induced by enhancement of apoptosis, autophagy manipulated through AKT/ERK signaling pathway. PMID: 30995142 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - April 19, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Central composite rotatable design for optimization of Budesonide loaded cross linked chitosan-dextran sulfate nanodispersion: Characterization, in vitro diffusion and aerodynamic study.
In conclusion, cross linked chitosan-dextran sulfate nanoparticles had properties suitable for nebulizable dispersion of increased drug loading, in vitro drug release and avoid the first pass effect. PMID: 30983428 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - April 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Design and development of a self-microemulsifying drug delivery system of Olmesartan Medoxomil for enhanced bioavailability.
Authors: Komesli Y, Ozkaya AB, Ergur BU, Kirilmaz L, Karasulu E Abstract 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 ...
Source: Drug Development and Industrial Pharmacy - April 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Development and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for curcumin transdermal delivery: an anti-inflammatory exposure.
Authors: Altamimi MA, Kaz M, Hadi Albgomi M, Ahad A, Raish M Abstract The purpose of this work is to develop novel lipid-based self-nanoemulsifying drug delivery systems (SNEDDS) as carriers for transdermal delivery of curcumin. SNEDDS containing black seed oil, medium chain mono- and diglycerides and surfactants, were prepared as curcumin delivery vehicles. Their formation spontaneity, morphology, droplet size, and drug loading were evaluated. Gel preparation containing two of the SNEDDS formulations were used in the carrageenan induced paw edema to evaluate the anti-inflammatory effect. Results showed droplet siz...
Source: Drug Development and Industrial Pharmacy - April 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Inhalable chitosan microparticles for simultaneous delivery of isoniazid and rifabutin in lung tuberculosis treatment.
Authors: Cunha L, Rodrigues S, Costa AMRD, Faleiro L, Buttini F, Grenha A Abstract The direct delivery of antibiotics to the lung has been considered an effective approach to treat pulmonary tuberculosis, which represents approximately 80% of total cases. In this sense, this work aimed at producing inhalable chitosan microparticles simultaneously associating isoniazid and rifabutin, for an application in pulmonary tuberculosis therapy. Spray-dried chitosan microparticles were obtained with adequate flow properties for deep lung delivery (aerodynamic diameter of 4 µm) and high drug association efficiencies (93...
Source: Drug Development and Industrial Pharmacy - April 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

The influence of storage relative humidity on aerosolization of co-spray dried powders of hygroscopic Kanamycin with the hydrophobic drug Rifampicin.
Authors: Momin MAM, Tucker IG, Das SC Abstract The purpose of this study was to investigate the influence of storage humidity on in vitro aerosolization and physicochemical properties of co-spray dried powders of kanamycin with rifampicin. The powders were stored for one-month in an open Petri dish at different relative humidities (RHs) (15%, 43% and 75%) and 25 ± 2 °C. The in vitro aerosolization (fine particle fraction, FPF) of the powders was determined by a next generation impactor (NGI). The moisture content, particle morphology and crystallinity of the powders were determined b...
Source: Drug Development and Industrial Pharmacy - April 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Anti-hyperuricemic property of 6-shogaol via self-microemulsifying drug delivery system in model rats: Formulation design, in vitro and in vivo evaluation.
Authors: Yang Q, Wang Q, Feng Y, Wei Q, Sun C, Firempong CK, Adu-Frimpong M, Li R, Bao R, Toreniyazov E, Ji H, Yu J, Xu X Abstract The prevalence of hyperuricemia is relatively high worldwide, and a great number of patients are suffering from its complications. 6-shogaol, an alkylphenol compound purified from the root of ginger (Zingiber officinale Roscoe), has been proved to possess the diverse pharmacological activities. However, its poor aqueous solubility usually lead to low bioavailability, and further clinical applications will be greatly discounted. The current study aimed to formulate a 6-shogaol-loaded-Sel...
Source: Drug Development and Industrial Pharmacy - April 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Nanoscaled pearl powder accelerates wound repair and regeneration in vitro and in vivo.
This study aims to investigate the effects and the underlying mechanism of the pearl powders with different particle sizes in wound treatment. Briefly, the pearl powder with different sizes was characterized for their particle sizes and morphology. The protein release profiles of these powders were also studied. The influence of the different size of pearl powder in the proliferation, migration of skin cells was evaluated. Then, with the rat skin excision model, the effect of pearl powder on wound repair and regeneration was investigated. It was demonstrated that, all the micro and nanosized pearl powders could both increa...
Source: Drug Development and Industrial Pharmacy - April 7, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

The preparation, characterization of Lupeol PEGylated Liposome and its functional evaluation in vitro as well as pharmacokinetics in rats.
CONCLUSION: The Lupeol-loaded PEGylated liposomes have successfully solved its poor hydrophilicity, low bioavailability. PMID: 30939950 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - April 4, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

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.
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 t...
Source: Drug Development and Industrial Pharmacy - April 3, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Design and Development of Bioinspired Calcium phosphate nanoparticles of MTX: Pharmacodynamic and Pharmacokinetic evaluation.
Authors: Pandey S, Mahtab A, Kumar V, Ahmad FJ, Verma AK, Talegaonkar S Abstract 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...
Source: Drug Development and Industrial Pharmacy - April 3, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Solubilization and determination of solution thermodynamic properties of itraconazole in different solvents at different temperatures.
Authors: Jagdale SK, Nawale RB Abstract 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 so...
Source: Drug Development and Industrial Pharmacy - April 3, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Synthesis and characterization of amphiphilic star-shaped copolymers based on β-cyclodextrin for micelles drug delivery.
CONCLUSION: The VP-loaded β-CD-P4 micelles exhibited controlled-release property, pH-induced feature and lung targeting capacity compared with VP injection, suggesting that the β-CD-P4 copolymers are an excellent candidate for micelles drug delivery. PMID: 30922119 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - March 31, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Formulation and optimization of intranasal nanolipid carriers of pioglitazone for the repurposing in Alzheimer's disease using Box-Behnken design.
The objective of the present study was to formulate and optimize intranasal (IN) nano lipid carriers (NLC) of PIO for its targeted delivery to the brain. A Box-Behnken design was employed to optimize the effect of three independent variables on two dependent variables. The optimized formulation had a particle size (PS) of 211.4 ± 3.54 nm and zeta potential of (ZP) of 14.9 ± 1.09 mv. The polydispersibility index (PDI) and entrapment efficiency (EE) was found to be 0.257 ± 0.108 and 70.18 ± 4.5% respectively. Storage stability s...
Source: Drug Development and Industrial Pharmacy - March 31, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Preparation and Evaluation of Optimized Zolmitriptan Niosomal Emulgel.
Authors: Mohamed MI, Abdelbary AA, Kandil SM, Mahmoud TM Abstract 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. METHODS: ...
Source: Drug Development and Industrial Pharmacy - March 30, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Preparation and in vitro/in vivo evaluation of azilsartan osmotic pump tablets based on the preformulation investigation.
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. The formulation of core tablet was optimized by orthogonal design and the release profiles ...
Source: Drug Development and Industrial Pharmacy - March 28, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Preparation, characterization and ex vivo-in vivo assessment of candesartan cilexetil nanocrystals via solid dispersion technique using an alkaline esterase activator carrier.
In conclusion, using of Tris as alkaline esterase activator carrier could be a promising tool to bypass the controversial effect of esterase enzymes that may be a source for inter-individual variations affecting ester prodrug candidates' efficacy. PMID: 30912678 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - March 28, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Green isolation and physical modification of pineapple stem waste starch as pharmaceutical excipient.
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. The SEM imaging showed morphological change with reduced surface roughness due to physical modification of the starch. Decreased crystallinity of modified starch (MPS) was confirmed by our XRD results: the peaks of A-t...
Source: Drug Development and Industrial Pharmacy - March 28, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Mannose functionalized plain and endosomolytic nanocomposite(s)-based approach for the induction of effective antitumor immune response in C57BL/6 mice melanoma model.
Authors: Sharma R, Vyas SP Abstract 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 ± 2.0 mV, respectively...
Source: Drug Development and Industrial Pharmacy - March 28, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Multivariate approaches for the development of quality control in-situ fiber optics dissolution methods for fixed-dose combination tablets.
Authors: Medendorp J, Colón I, Ryan T Abstract 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. These obstacles might render FO dissolution method dev...
Source: Drug Development and Industrial Pharmacy - March 25, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Chitosan-TPP Nanoparticles Stabilized by Poloxamer for Controlling the Release and Enhancing the Bioavailability of Doxazosin Mesylate: In Vitro, and In Vivo Evaluation.
CONCLUSIONS: The study proved that controlling the release of DM from NPs enhance its bioavailability and improve the compliance of patients with hypertension or benign prostatic hyperplasia. PMID: 30884977 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - March 21, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect.
Authors: Choi Y, Min KA, Kim CK Abstract 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 ...
Source: Drug Development and Industrial Pharmacy - March 21, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Novel hypolipidemic conjugates of fatty acid and bile acid with lysine for linkage.
Authors: Jin XY, Zhu CB, Fan SY, Sun JL, Shi YC, Wang CH, Wang HF, Zhong BH, Yao YS, Shi WG Abstract 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...
Source: Drug Development and Industrial Pharmacy - March 21, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Fabrication of solid lipid nanoparticles of lurasidone HCl for oral delivery: Optimization, in vitro characterization, cell line studies and in vivo efficacy in schizophrenia.
CONCLUSION: It was concluded that oral administration of LH-SLNs in rats improved the bioavailability of LH via lymphatic uptake along with improved therapeutic effect in MK-801 induced schizophrenia model in rats. PMID: 30880488 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - March 20, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Solubility advantage of sulfanilamide and sulfacetamide in natural deep eutectic systems: experimental and theoretical investigations.
CONCLUSIONS: The obtained results show the feasibility of using NADES as solubility enhancers for sulfonamides and encourage for further exploration in this field. PMID: 30883240 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - March 20, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Cubosomal based Oral Tablet for controlled Drug Delivery of Telmisartan: Formulation, in-vitro Evaluation and in-vivo Comparative Pharmacokinetic Study in Rabbits.
Authors: Yasser M, Teaima M, El-Nabarawi M, Abd El-Monem R Abstract A nanoparticulate system; cubosomes has been suggested to support the controlled release of Telmisartan (TEL), a poorly water-soluble medication. Four distinctive formulae were selected according to the results of three estimated responses. The liquid cubosomes were successfully adsorbed onto aerosil 380 to form granules. The formulae were evaluated for their flow properties. The best granules were compressed into tablets suitable for oral administration. The tablets were evaluated for its performance. The in vivo study of the best selected cubosom...
Source: Drug Development and Industrial Pharmacy - March 14, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Correction.
Authors: PMID: 30794030 [PubMed - in process] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - February 24, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research