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Drug Development and Industrial Pharmacy

Pratibha Auti, Satish Gabhe, Kakasaheb Mahadik
Piperine has been widely used as a bioenhancer. Simvastatin belongs to a group of medicines known as statins. It acts by inhibiting HMG CoA reductase and acts primarily as a hypolipidemic agent. In this study some derivatives of Piperine were synthesized. They were studied for their bioenhencing effect [10mg/kg] and this effect was compared with that of Piperine. The pharmacokinectic profile of Simvastatin alone and in combination with Piperine and Piperine derivatives were investigated by validated HPLC method as per USFDA guidelines...
January 16, 2019: Drug Development and Industrial Pharmacy
Simone Jacobus Berlitz, Damiê De Villa, Luiz Augusto Maschmann Inácio, Samuel Davies, Kelly Cristine Zatta, Silvia Stanisçuaski Guterres, Irene Clemes Külkamp-Guerreiro
OBJECTIVE: to develop an azelaic acid (AzA)-loaded nanoemulsion with hyaluronic acid (HA) as a double targeting strategy to increase drug retention and tyrosinase inhibition activity. SIGNIFICANCE: dermic melasma is a recalcitrant disease. Therefore, the development of new technologies that allow a deeper penetration in the skin while enhancing the efficacy of a safe and well-known dermatological active, like AzA, is a very promising alternative to improve the treatment of this disease...
January 15, 2019: Drug Development and Industrial Pharmacy
Hira Ijaz, Ume Ruqia Tulain, Farooq Azam, Junaid Qureshi
Current research work conducted to synthesize Thiol modifiedarabinoxylan and its application in fabrication of hydrogel. Thioglycolic acid was esterified with arabinoxylan to prepare Thiolatedarabinoxylan. Appearance of peak at 2533.34cm-1 in FTIR and thiol content showed successful thiolation. pH dependent Thiolatedarabinoxylan/acrylic acid(TAX/AA) hydrogels of perindopril erbumine was prepared via free-radical co-polymerization. Perindopril erbumine (PE) was employed as model drug. Different bathes with different feed ratio of TAX, AA and MBA were prepared and their influence on swelling, solvent penetration and consequent drug release was investigated...
January 14, 2019: Drug Development and Industrial Pharmacy
Zahra Karami, Mohammad Reza Saghatchi Zanjani, Saeed Rezaee, Kobra Rostamizadeh, Mehrdad Hamidi
OBJECTIVE: Indinavir (IDV), an antiretroviral protease inhibitor used in treatment of HIV infection, has limited entry into brain due to efflux by the P-glycoprotein presented in blood-brain barrier. The aim of present study was to develop lactoferrin-treated nanoemulsion containing indinavir (Lf-IDV-NEs) for delivery to brain. METHODS: Indinavir-loaded nanoemulsions (IDV-NEs) were prepared by high-speed homogenization method, and then lactoferrin was coupled to IDV-NEs by water soluble EDC method...
January 14, 2019: Drug Development and Industrial Pharmacy
Manal K M Darwish, Amal S M Abu El-Enin, Kamilia H A Mohammed
The main objective of this research is to formulate, optimize and evaluate raft forming chewable tablets of Nizatidine. Various raft-forming agents were used in preliminary screening. Sodium alginate showed maximum raft strength, so tablets were prepared using sodium alginate as the raft forming agent, along with calcium carbonate (CaCO3 ) as antacid and raft strengthening agent, and sodium bicarbonate (NaHCO3 ) as a gas generating agent. RESEARCH DESIGN AND METHODS: Raft forming chewable tablets containing Nizatidine were prepared by direct compression and wet granulation methods, and evaluated for drug content, acid neutralization capacity, raft strength, and in- vitro drug release in 0...
January 14, 2019: Drug Development and Industrial Pharmacy
Rezvan Yazdian-Robati, Atefeh Arab, Mohammad Ramezani, Houshang Rafatpanah, Amirhossein Bahreyni, Maryam Sadat Nabavinia, Khalil Abnous, Seyed Mohammad Taghdisi
To explore the effect of combination therapy of epirubicin (Epi) and melittin (Mel) to cancer cells, calcium carbonate nanoparticles (CCN), as carriers, were developed which were modified with MUC1-Dimer aptamers as targeting agents. Both Epi and Mel were delivered at the same time to cancer cells overexpressing the target of MUC1 aptamer, mucin 1 glycoproteins (MCF7 and C26 cells). CCN were prepared with a water-in-oil emulsion method. Epi and Mel were separately encapsulated in CCN and the nanoparticles were modified with MUC1-Dimer aptamers...
January 11, 2019: Drug Development and Industrial Pharmacy
V Rastogi, P Yadav, A Husain, A Verma
OBJECTIVE: Innovations in material science, has made it possible to fabricate a pharmaceutical material of modifiable characteristics and utility, in delivering therapeutics at a sustained/controlled rate. The objective of this study is to design and optimize the controlled release transdermal films of S-Amlodipine besylate by intercalating hydrophilic and hydrophobic polymers. METHODS: 3(2) factorial design and response surface methodology was utilized to prepare formulations by intercalating the varied concentration of polymers(A) and penetration enhancer(B) in solvent...
January 11, 2019: Drug Development and Industrial Pharmacy
Maimoona Qindeel, Naveed Ahmed, Fakhara Sabir, Samiullah Khan, Asim Ur Rehman
OBJECTIVE: Difference of pH that exists between the skin surface and blood circulation can be exploited for transdermal delivery of drug molecules by loading drug into pH-sensitive polymer. Eudragit S100 (ES100), a pH-sensitive polymer having dissolution profile above pH 7.4, is used in oral, ocular, vaginal and topical delivery of drug molecules. However, pH-sensitive potential of this polymer has not been explored for transdermal delivery. The aim of this research work was to exploit the pH-sensitive potential of ES100 as a nanocarrier for transdermal delivery of model drug i...
January 11, 2019: Drug Development and Industrial Pharmacy
Sonia Mendoza-Cardozo, Luis D Pedro-Hernández, Ulises Organista-Mateos, Luis Isaac Allende-Alarcón, Elena Martínez-Klimova, Teresa Ramírez-Ápan, Marcos Martínez-García
A possible way of improving the activity and selectivity profile of antitumor agents is to design drug carrier systems employing soluble macromolecules. Thus, four resorcinarene-PAMAM-dendrimer conjugates of chlorambucil with different groups in the lower part of the macrocycle and different length dendritic arms showed a good stability of the chemical link between drug and spacer. Evaluation of the cytotoxicity of the resorcinarene-PAMAM-dendrimer-chlorambucil conjugate employing a sulforhodamine B (SRB) assay in K-562 (human chronic myelogenous leukemia cells) demonstrated that the conjugate was more potent as an antiproliferative agent than chlorambucil...
January 11, 2019: Drug Development and Industrial Pharmacy
Priya Shah, Sadhana J Rajput
In the present work, MCM-41 and MCM-48 type of nanoparticles were successfully engineered. Effect of nanosize and amine functionalization on drug release, in vitro intestinal absorption and in vivo pharmacokinetic behavior was investigated in a comprehensive manner. The tailor made bare and surface decorated MCM-41 and MCM-48 were synthesized and evaluated for their mesoporous skeleton, pore size, particle size, surface area, zeta potential etc. by nitrogen sorption, DLS, TEM etc. Incorporation of raloxifene (RLF) was affirmed using optimized immersion-solvent evaporation technique and its success confirmed by DSC, IR and XRD analysis...
January 11, 2019: Drug Development and Industrial Pharmacy
Dan Lou, Xiao Cui, Bao Su-Su, Wei Sun, Wen-He Pan, Meng-Chun Chen, Yao-Yao Dong, Guo-Xin Hu, Chen Rui-Jie, Zhe Wang
We investigated the effect of azole antifungal drugs (ketoconazole, voriconazole, and itraconazole) on the pharmacokinetics of apatinib in rats. The rats in ketoconazole, voriconazole, and itraconazole groups received single-dose apatinib 30mg/kg after the oral administration of ketoconazole, voriconazole, and itraconazole, respectively. Co-administration of ketoconazole or voriconazole significantly increased the apatinib Cmax and AUC(0-t) and decreased the clearance. Co-administration of itraconazole did not significantly affect the pharmacokinetics parameters of apatinib...
January 11, 2019: Drug Development and Industrial Pharmacy
Adeeba Jamil, Mohd Aamir Mirza, Khalid Anwer, Pragya S Thakur, SaadM Alshahrani, Abdullah S Alshetaili, Sushama Telegaonkar, Amulya K Panda, Zeenat Iqbal
Despite the ongoing extensive research, cancer therapeutics still remains an area with unmet needs which is hampered by shortfall in the development of newer medicines. The present study discusses a nano-based combinational approach for treating solid tumor. Dual loaded nanoparticles encapsulating gemcitabine HCl (GM) and simvastatin (SV) was fabricated by double emulsion solvent evaporation method and optimized. Optimized nanoparticles showed a particle size of 258 ± 2.4 nm, PDI of 0.32 ± 0.052 and zeta potential of -12...
January 11, 2019: Drug Development and Industrial Pharmacy
Phatsawee Jansook, Zoltán Fülöp, Garnpimol C Ritthidej
Amphotericin B (AmB) is one of the most effective systemic antifungal agents, but its use is circumscribed by the dose-limiting toxicity of the conventional micellar dispersion formulation, Fungizone®. Significantly lesser toxicity is obtained when AmB incorporated into the aqueous dispersion of lipid nanoparticles. The aim of this study was to develop and characterize AmB loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). NLC differed from SLN by the presence of liquid lipid, glyceryl tri(caprylate/caprate) in the lipid matrix...
January 11, 2019: Drug Development and Industrial Pharmacy
Harani Avasarala, Sathis Kumar Dinakaran, Ravishankar Kakaraparthy, Vijaya Ratna Jayanti
Self emulsifying drug delivery systems (SES) were developed to improve oral bioavailability of asenapine maleate (ASM), an antipsychotic drug with challenging amphiphobic nature and extensive pre-systemic metabolism.ASM-SES was prepared by choosing the proportion of oil, surfactant, co-surfactant from constructed phase diagram. The in vitro and ex vivo evaluation was done. In vivo evaluation was done through pharmacokinetic and pharmacodynamic studies. Role of lymphatic absorption was studied by lymphatic absorption inhibition study...
January 9, 2019: Drug Development and Industrial Pharmacy
Luke Schenck, Athanas Koynov, Aaron Cote
Direct compression offers a simple route to generate pharmaceutical dosage units and is core to the growing arena of continuous manufacturing. However, direct compression can be untenable for some active materials. This paper will outline three specific challenges API's can present to direct (active pharmaceutical ingredients) compression. The first involves API's having exceedingly high aspect ratio ("needles") or small particle size resulting in low bulk density and poor flow properties. Two additional cases are relatively newer challenges to direct compression driven by the growing need for solubility enhancing formulations, and involve nano-crystalline materials and spray dried amorphous dispersions...
January 4, 2019: Drug Development and Industrial Pharmacy
Arehalli S Manjappa, Rayasa S Ramachandra Murthy
PURPOSE: To prepare 7-epidocetaxel (7ED) and 10-oxo-7-epidocetaxel (10-O-7ED) formulations as like marketed Taxotere® (TXT) injection and to screen them for in vitro and in vivo anticancer efficacy including their in vivo toxicity behavior. METHODS: The 7ED and 10-O-7ED formulations were screened for in vitro anti-proliferative, anti-metastatic and cell cycle arresting behaviors. Further, in vivo acute toxicity of TXT injection containing 10% of 7ED and 10-O-7ED separately and the therapeutic study of 10-O-7ED alone were studied in B16F10 experimental metastasis mouse model...
January 1, 2019: Drug Development and Industrial Pharmacy
Seema Saroj, Sadhana J Rajput
It is a challenge to deliver therapeutics exclusively to cancer cells, while sparing the normal cells. However, pH sensitive delivery systems have proved to be highly efficient in fulfilling this task due to their ability to provide on demand and selective release of drug at acidic tumor sites. As a proof of concept, here pH responsive drug delivery system based on mesoporous core shell nanoparticles (NPs) surrounded with poly acrylic acid (PAA) layers were prepared employing a facile synthesis strategy. Bicalutamide (BIC) was encased into surface functionalized MCM-41 nanoparticles via electrostatic interactions...
December 24, 2018: Drug Development and Industrial Pharmacy
Mohammed M Mehanna, Mohamad Ibrahim Shabarek, H A El-Maradni
Pravastatin is a promising drug utilized in the treatment of hyperlipidemia, yet, its main clinical limitation is due to gastric liability which fractions its oral bioavailability to less than 18%. The purpose of the current study is to encapsulate pravastatin into Eudragit®-based spray-dried microparticles aspiring to overcome its acid liability. With the aim to optimize the microparticles, formulation and process parameters were studied through acid resistance challenging test. Physicochemical characterization of the optimized spray-dried pH sensitive microparticles namely; in-vitro dissolution, surface morphology, compatibility and solid-state studies were performed...
December 21, 2018: Drug Development and Industrial Pharmacy
Chau Tm Tran, Phuong Hl Tran, Thao Td Tran
The objective of this study was to achieve an optimal formulation of hydrophilic-hydrophobic conjugates for nano-sized solid dispersions (SDs) with enhanced dissolution of multiple drugs in different gastrointestinal (GI) tract environments. A new conjugate powder with an optimized process was used to fabricate SDs that contained three poorly water-soluble drugs that were also poorly soluble in different dissolution media. The self-assembled nanoparticle formation, drug crystallinity and SD molecular interactions were investigated by measuring the particle size during dissolution testing and physicochemical property analysis (powder X-ray diffraction and Fourier transform infrared spectroscopy)...
December 21, 2018: Drug Development and Industrial Pharmacy
Hai-Qiu Ma, Ying Wang, Yong-Hong Mao, Shu-Yan Wang, Yu-Pu Zhang, Chen-Qiang Zuo, Shao-Juan Liang, Jun-Wei Liu
BACKGROUND: Hand-Foot-Mouth Disease may cause severe central nervous system complications and even death, that induced mainly by enterovirus 71 (EV71), which is a non-enveloped virus. Inactivation of the EV71on hands could effectively inhibit the transmission. However, the inactivations of the EV71by conventional disinfectants including the alcohols are poor, due to the high stability of the EV71. A novel pyridyl imidazolidinone compound (TJAB1099), was designed to specifically inhibit EV71replication in vitro...
December 21, 2018: Drug Development and Industrial Pharmacy
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