Abhishek Gir, Rinkee Verma*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh, E-mail: [email protected]
Oral bioavailability of a drugdepends on its solubility and/or dissolution rate, therefore efforts to increase dissolution of drugs with limited water solubility is often needed.Improving oral bioavailability of drugs those given as solid dosage forms remains a challenge for the formulation scientists due to solubility problems. The dissolution rate could be the rate-limiting process in the absorption of a drug from a solid dosage form of relatively insoluble drugs. By improvement of drug release profiles of these drugs, it is possible to improve its bioavailability andreduce side effects. When delivering an active agent orally,it must first dissolve in gastric fluids and/or intestinal fluids before it can then permeate the membranes of (GI) gastro intestinal tract to reach systemic circulation.
Durgeshwari Swarnkar, Sanjay Mire*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh, E-mail: [email protected]
For most molecule-targeted anticancer systems, intracellular protein targets are very difficult to be accessed by antibodies, and also most efforts are made to inhibit protein activity temporarily rather than inactivate them permanently. In this work we firstly designed and synthesized multifunctional polymer-drugconjugates for intracellular molecule-targeted binding and inactivation of protein for growth inhibition of cancer cells. Small molecule drug was conjugated to polymer side chain for intracellular signal protein targeting, and simultaneously the fluorescent characteristic of polymer for tracing the cellular uptake and localization of polythiophene-drug conjugates by cell imaging.
Rahul Choubey, Shashikant Sahu*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh, E-mail: [email protected]
The world is facing a burden of infectious diseases like measles, swine flu, acute respiratory infections, typhoid and tuberculosis. Among them most common problem is bronchiolitis and pneumonia which is caused by human respiratory syncytical virus (HRSV). Despite of intensive research over the decades, medical therapy has remained unchanged and controversial. Human respiratory syncytical virus (HRSV) belongs to the family paramyxoviridae. In the present review, earlier attempts for HRSV vaccine discovery and modern treatment option for HRSV infection by reverse vaccinology (RV) approach is discussed, which helps in systematic analysis of sequences, structure and interaction of the proteins involved in virus life cycle and stimulating protective immunity.
Shradha Dwivedi, Pravin Sao*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Science and Research, Kohka-Kurud Road, Bhilai-490024(Chhattisgarh), E-mail: [email protected]
Buccal administration of drug provides a convenient route of administration for both systemic and local drug actions. The preferred site for retentive oral transmucosal delivery systems and for sustained and controlled release delivery device is the buccal mucosa. Rapid developments in the field of molecular biology and gene technology resulted in generation of many macromolecular drugs including peptides, proteins, polysaccharides and nucleic acids in great number possessing superior pharmacological efficacy with site specificity and devoid of untoward and toxic effects. However, the main impediment for the oral delivery of such drugs as potential therapeutic agents is their extensive presystemic metabolism, instability in acidic environment resulting into inadequate and erratic oral absorption.
Tikesh Kumar Banothe, Siddharth Kumar*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Kohka-Kurud Road, Bhilai – 490024 (Chhattisgarh), E-mail: [email protected]
Several methods and techniques are potentially useful for the preparation of Microparticles in the field of controlled drug delivery. The type and the size of the microparticles, the entrapment, release characteristics and stability of drug in microparticles in the formulations are dependent on the method used. One of the most common methods of preparing microparticles is the single emulsion technique. Poorly soluble, lipophilic drugs are successfully retained within the microparticles prepared by this method. However, the encapsulation of highly water soluble compounds including protein and peptides presents formidable challenges to the researchers.
Dhanendra Sahu, Vikas Kant Kurre*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Kohka-Kurud Road, Bhilai – 490024 (Chhattisgarh), E-mail: [email protected]
The different types rubber are used in pharmaceutical packaging e.g. butyl rubber, nitrile rubber, chloroprene rubber, silicon rubber. The variation should be minimized to apply fragmentations and self-sealing test in pharmaceutical rubber closure.The fragmentation test is used to compare with another rubber closure to number of fragment found in water with the help of piercing with the hypodermic syringe. After the fragmentation test it was seen that number of fragment in water where found to be higher in case of natural rubber as compare to latex rubber which indicates that latex rubber is best as closure for aqueous preparation . The self – sealing test was performed on few sample of natural rubber closure.
Garima Sharma, Mithlesh Ojha*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Kohka-Kurud Road, Bhilai – 490024 (Chhattisgarh), E-mail: [email protected]
Aquasome are colloidal range biodegradable novel drug delivery carrier based on the principle of self assembly. Administration of bioactive molecules in their active state has been an enormous task to the pharmaceutical additionally as biotechnological industries. The pharmaceutical & biotechnological industry have challenges to maked an appropriate route of drug delivery system. Recent advancement within the space of biotechnology & genetics science has resulted in promotion of protein & peptides are therapeutic agent. The main goal of drug delivery system to optimized drug loading & release properties for long self life& low toxicity. NDDS are considered as promising carrier for broad range of drug delivery system.
Alok Singh Thakur*, Ravitas Deshmukh, P. Sudhir Kumar
Faculty of Pharmaceutical Sciences, SSGI, SSTC, Junwani, Bhilai, C.G., India
School of Pharmaceutical Sciences, Soa University, Bhubaneswar, Odhisha, India, Tel: 09752097870; E-mail: [email protected]
A new series of 3-(4-substitutedphenyl)-1-(4-(4,6-dimethyl-6H-1,3-thiazin-2-yl)phenylsulfonyl)-1-substitutedlurea (5a-o) was prepared and established by spectroscopic and analytical methods. This route of synthesis is proved to be easy and effectual which makes it possible to explore the novel site for substitution in sulfonylurea as well as the way of thiazine can be prepared. Rational of trisubtitution in sulfonylurea derivatives was achieved by protecting the ionizable amine by various aromatic and heterocyclic molecules.
Amit Alexander*, Swarnlata Saraf, Shailendra Saraf
University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, 492010, E-mail: [email protected]
In the present study, we have investigated the role of thermoreversible injectable hydrogel for the successful administration of a PEGylated anticancer drug. To achieve the objective, a modified PEGylated melphalan (MLPEG) synthesized from a linear methoxy poly (ethylene glycol) (M-PEG) 2000 and 5000, Da with improved solubility was loaded to the thermosensitive Poloxamer 407 (P407) gel to produce an injectable hydrogel (MPX). As far as the safety issues are concern, conjugates at a concentration of 32 µg/ml after 1 h, showed low hemolysis (48.8 ± 1.5%) compared to high hemolysis (81.3 ± 0.5) for MLPEG 5000 and MLPEG 2000, respectively. Therefore, a significant decrease in hemolytic activity was found in case of MLPEG 5000 conjugate compared to MLPEG 2000.
Nanoparticles have several biomedical and industrial applications in diagnosis of disease, targeted chemotherapy and in drug delivery. Multifunctionality and sub-micronic size is the main characteristics of nanoparticles. Nanoparticles can be integrated with ligands, imaging labels, therapeutic agents and other functionalities for site specific drug delivery and cellular uptake. In the present review we are discussing the application and synthesis of gold nanoparticles which is the most studied among all metallo-nanoparticles. Various anticancer drugs are available but these are cause the necrosis of cancerous cell as well as normal cells. But gold nanoparticles cause the necrosis of only cancer cells.
A Technique to Improve the Bioavailabiligy of Poorly Water Soluble Drugs: Solid Dispersion
Abhishek Gir, Rinkee Verma*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh, E-mail: [email protected]Oral bioavailability of a drugdepends on its solubility and/or dissolution rate, therefore efforts to increase dissolution of drugs with limited water solubility is often needed.Improving oral bioavailability of drugs those given as solid dosage forms remains a challenge for the formulation scientists due to solubility problems. The dissolution rate could be the rate-limiting process in the absorption of a drug from a solid dosage form of relatively insoluble drugs. By improvement of drug release profiles of these drugs, it is possible to improve its bioavailability andreduce side effects. When delivering an active agent orally,it must first dissolve in gastric fluids and/or intestinal fluids before it can then permeate the membranes of (GI) gastro intestinal tract to reach systemic circulation.
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Development Prospects of Polymer Conjugation for the Inhibition of Cancer Cells
Durgeshwari Swarnkar, Sanjay Mire*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh, E-mail: [email protected]For most molecule-targeted anticancer systems, intracellular protein targets are very difficult to be accessed by antibodies, and also most efforts are made to inhibit protein activity temporarily rather than inactivate them permanently. In this work we firstly designed and synthesized multifunctional polymer-drugconjugates for intracellular molecule-targeted binding and inactivation of protein for growth inhibition of cancer cells. Small molecule drug was conjugated to polymer side chain for intracellular signal protein targeting, and simultaneously the fluorescent characteristic of polymer for tracing the cellular uptake and localization of polythiophene-drug conjugates by cell imaging.
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Advancement in the Viral Vaccine for HRSV by Reverse Vaccinology
Rahul Choubey, Shashikant Sahu*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh, E-mail: [email protected]The world is facing a burden of infectious diseases like measles, swine flu, acute respiratory infections, typhoid and tuberculosis. Among them most common problem is bronchiolitis and pneumonia which is caused by human respiratory syncytical virus (HRSV). Despite of intensive research over the decades, medical therapy has remained unchanged and controversial. Human respiratory syncytical virus (HRSV) belongs to the family paramyxoviridae. In the present review, earlier attempts for HRSV vaccine discovery and modern treatment option for HRSV infection by reverse vaccinology (RV) approach is discussed, which helps in systematic analysis of sequences, structure and interaction of the proteins involved in virus life cycle and stimulating protective immunity.
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Buccal Patches: Advancement in Oral Drug Delivery System
Shradha Dwivedi, Pravin Sao*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Science and Research, Kohka-Kurud Road, Bhilai-490024(Chhattisgarh), E-mail: [email protected]Buccal administration of drug provides a convenient route of administration for both systemic and local drug actions. The preferred site for retentive oral transmucosal delivery systems and for sustained and controlled release delivery device is the buccal mucosa. Rapid developments in the field of molecular biology and gene technology resulted in generation of many macromolecular drugs including peptides, proteins, polysaccharides and nucleic acids in great number possessing superior pharmacological efficacy with site specificity and devoid of untoward and toxic effects. However, the main impediment for the oral delivery of such drugs as potential therapeutic agents is their extensive presystemic metabolism, instability in acidic environment resulting into inadequate and erratic oral absorption.
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Double Emulsion Technique for Preparation of Microparticle as Controlled Drug Delivery System
Tikesh Kumar Banothe, Siddharth Kumar*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Kohka-Kurud Road, Bhilai – 490024 (Chhattisgarh), E-mail: [email protected]Several methods and techniques are potentially useful for the preparation of Microparticles in the field of controlled drug delivery. The type and the size of the microparticles, the entrapment, release characteristics and stability of drug in microparticles in the formulations are dependent on the method used. One of the most common methods of preparing microparticles is the single emulsion technique. Poorly soluble, lipophilic drugs are successfully retained within the microparticles prepared by this method. However, the encapsulation of highly water soluble compounds including protein and peptides presents formidable challenges to the researchers.
Download PDF to Continue...
Evaluation of Self – Sealling Capacity & Fragmentation Test for Rubber Closure of Pharmaceutical Importance
Dhanendra Sahu, Vikas Kant Kurre*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Kohka-Kurud Road, Bhilai – 490024 (Chhattisgarh), E-mail: [email protected]The different types rubber are used in pharmaceutical packaging e.g. butyl rubber, nitrile rubber, chloroprene rubber, silicon rubber. The variation should be minimized to apply fragmentations and self-sealing test in pharmaceutical rubber closure.The fragmentation test is used to compare with another rubber closure to number of fragment found in water with the help of piercing with the hypodermic syringe. After the fragmentation test it was seen that number of fragment in water where found to be higher in case of natural rubber as compare to latex rubber which indicates that latex rubber is best as closure for aqueous preparation . The self – sealing test was performed on few sample of natural rubber closure.
Download PDF to Continue...
Carrier System for Self-Assembling Supramolecular & Nanoparticular System
Garima Sharma, Mithlesh Ojha*, Ajazuddin, Amit Alexander, D. K. Tripathi
Rungta College of Pharmaceutical Sciences and Research, Kohka-Kurud Road, Bhilai – 490024 (Chhattisgarh), E-mail: [email protected]Aquasome are colloidal range biodegradable novel drug delivery carrier based on the principle of self assembly. Administration of bioactive molecules in their active state has been an enormous task to the pharmaceutical additionally as biotechnological industries. The pharmaceutical & biotechnological industry have challenges to maked an appropriate route of drug delivery system. Recent advancement within the space of biotechnology & genetics science has resulted in promotion of protein & peptides are therapeutic agent. The main goal of drug delivery system to optimized drug loading & release properties for long self life& low toxicity. NDDS are considered as promising carrier for broad range of drug delivery system.
Download PDF to Continue...
Synthesis and Characterization of Trisubstituted Sulfonylurea Derivatives Containing Thiazine
Alok Singh Thakur*, Ravitas Deshmukh, P. Sudhir Kumar
Faculty of Pharmaceutical Sciences, SSGI, SSTC, Junwani, Bhilai, C.G., IndiaSchool of Pharmaceutical Sciences, Soa University, Bhubaneswar, Odhisha, India, Tel: 09752097870; E-mail: [email protected]
A new series of 3-(4-substitutedphenyl)-1-(4-(4,6-dimethyl-6H-1,3-thiazin-2-yl)phenylsulfonyl)-1-substitutedlurea (5a-o) was prepared and established by spectroscopic and analytical methods. This route of synthesis is proved to be easy and effectual which makes it possible to explore the novel site for substitution in sulfonylurea as well as the way of thiazine can be prepared. Rational of trisubtitution in sulfonylurea derivatives was achieved by protecting the ionizable amine by various aromatic and heterocyclic molecules.
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Melphalan Loaded In situ Thermoreversible Injectable Hydrogel of Tri Block Copolymer System
Amit Alexander*, Swarnlata Saraf, Shailendra Saraf
University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, 492010, E-mail: [email protected]In the present study, we have investigated the role of thermoreversible injectable hydrogel for the successful administration of a PEGylated anticancer drug. To achieve the objective, a modified PEGylated melphalan (MLPEG) synthesized from a linear methoxy poly (ethylene glycol) (M-PEG) 2000 and 5000, Da with improved solubility was loaded to the thermosensitive Poloxamer 407 (P407) gel to produce an injectable hydrogel (MPX). As far as the safety issues are concern, conjugates at a concentration of 32 µg/ml after 1 h, showed low hemolysis (48.8 ± 1.5%) compared to high hemolysis (81.3 ± 0.5) for MLPEG 5000 and MLPEG 2000, respectively. Therefore, a significant decrease in hemolytic activity was found in case of MLPEG 5000 conjugate compared to MLPEG 2000.
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Futuristic Applications of Gold Nanoparticles
Apurva Yadav*, Jharna Deshmukh, Swarnali Das Paul
Faculty of pharmaceutical sciences Shri Shankaracharya Technical Campus Junwani Bhilai, Tel: 8359094642; E-mail: [email protected]Nanoparticles have several biomedical and industrial applications in diagnosis of disease, targeted chemotherapy and in drug delivery. Multifunctionality and sub-micronic size is the main characteristics of nanoparticles. Nanoparticles can be integrated with ligands, imaging labels, therapeutic agents and other functionalities for site specific drug delivery and cellular uptake. In the present review we are discussing the application and synthesis of gold nanoparticles which is the most studied among all metallo-nanoparticles. Various anticancer drugs are available but these are cause the necrosis of cancerous cell as well as normal cells. But gold nanoparticles cause the necrosis of only cancer cells.
Download PDF to Continue...