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(Ramesh Chand Nagarwal)
Mr. Ramesh Chand Nagarwal, Senior Research Fellow, Department of Pharmaceutical Engineering, IT-BHU presented his research Paper on “Chitosan Coated Sodium alginate Nanoparticles for Ophthalmic Delivery” in AAPS National Biotechnology Conference, held from 16-19 May 2010 at San Francisco, California, USA.
Financial assistance was given by CSIR (Council of Scientific and Industrial Research) and BHU. He also received travel award from the AAPS Formulation Design and Development Section to attend the conference.
Currently, Ramesh is perusing PhD in the field of Nanoparticulate systems for Ophthalmic Delivery under the supervision Prof. J. K. Pandit. In December 3-6, 2009, he has also presented his research paper on “5-FU loaded PLA nanoparticles for topical treatment of conjunctival/corneal squamous cell carcinoma”, in the 8th International Symposium on Ocular Pharmacology and Therapeutics, held at Rome, Italy.
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About authors:
*Ramesh Chand Nagarwal
Research Scholar, Department of Pharmaceutical Engineering, IT-BHU
Email: rcnagarwal.rs.phe@itbhu.ac.in, ramesh_itbhu79@yahoo.co.in
*Prof. J. K. Pandit
Professor, Department of Pharmaceutical Engineering, IT-BHU
Email: jkpandit@bhu.ac.in, dr.jkpandit@gmail.com
Background of research (by Ramesh Chand Nagarwal):
Drug loaded polymeric nanoparticles (DNPs) offer several favorable biological properties, such as biodegradability, nontoxicity, biocompatibility and mucoadhesiveness. Various efforts in ophthalmic drug delivery have been made to improve the bioavailability and to prolong the residence time of drugs applied topically onto the eye. These submicron particles are better than conventional ophthalmic dosage forms to enhance bioavailability without blurring the vision. Based on this concept, the chitosan coated and polylactic acid loaded 5-FU were fabricated by simple techniques with better physical stability for the treatment of conjunctival/corneal squamous cell carcinoma in the eye. This unique combination of properties makes DNPs a novel polymeric drug delivery device, which fulfils the requirements for ophthalmic application.
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Educational Background of Ramesh Chand Nagarwal
2007-Present: Ph.D. pursuing (Pharmaceutics), Department of Pharmaceutics, IT, Banaras Hindu University, Varanasi-221005, U.P, India
2004-2006: M. Pham (Pharmaceutics), Department of Pharmaceutics, IT, Banaras Hindu University, Varanasi-221005, India
1999-2004: B. Pharm., Lachoo Memorial College of Science & Technology, Jodhpur, Rajasthan, India.
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http://www.aapsj.org/abstracts/NBC_2010/NBC10-000284.PDF
Chitosan Coated Sodium alginate Nanoparticles for Ophthalmic Delivery
Purpose
The objective of the investigation was to develop sodium alginate (SA) nanoparticles loaded 5-FU (SA-DNPs) for ophthalmic delivery.
Methods
Nanoparticles were prepared by gelation technique. Briefly, Chitosan solution (CH) (0.05 to 0.1 %w/v) was added to SA solution (0.03 to 0.05% w/v) containing 5-FU followed by stirring for 30 min. The opalescent dispersion was stored overnight and separated by cooling centrifugation; final pellet was redispersed in CH and stirred for 30 min, re-centrifuged and lyophilized. DNPs were characterized by dynamic light scattering, scanning electron microscopy, atomic force microscopy, and Zeta potential. The encapsulation efficiency and loading capacity of DNPs were analyzed by UV & HPLC methods. The in-vitro release of SA-DNPs was studied by dialysis membrane method. Ocular tolerability was tested by HETCEM method. Effect of pH, mass ratio of SA/CH and size of DNPs on stability of colloidal system were studied.
Results
The size and drug encapsulation efficiency were dependent on molar ratio of SA and CH. Stability of the colloidal system was influenced by size and Zeta potential of DNPs. The size range 400 to 600 nm of SA-DNPs and zeta potential was increased by coating with chitosan that is desirable to increase the stability of the colloidal system. The 5-FU loaded SADNPs presented a sustained release of 5-FU compared to the 5-FU solution. SA-DNPs were shown to be non-irritant by HET-CAM test. The result obtained in this study suggests that 5-FU loaded nanoparticles could be further evaluated for pharmacokinetic study in rabbit eye.
Conclusion
SA-DNPs were prepared and characterized. Results showed sustained release of 5-FU from nanoparticles, and optimum size and zeta potential were appropriate for the stability of nanosuspension. Ocular administration of 5-FU in the form of mucoadhesive SA-DNPs can be expected to increase the time of drug residence on the eye surface, increasing drug bioavailability and prolonging the pharmacological effect. These SA-DNPs may be effective in eradicating conjunctival/corneal squamous cell carcinoma by topical chemotherapy.
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About AAPS Journal
About The AAPS Journal
The AAPS Journal (ISSN 1550-7416) is an online-only journal publishing peer-reviewed scholarly reviews, themed issues and research articles within the entire scope of the pharmaceutical sciences encompassed by the AAPS membership. The Journal particularly aims to foster the dissemination of scientific information presented at AAPS-sponsored meetings, workshops and symposia, through the publication of invited reviews in themed issues. Additionally, guest editors are invited to organize special themed issues on scientific subjects of current interest. Submission of uninvited expert reviews and research articles in all areas of pharmaceutical sciences are welcomed, although manuscripts focused on pharmaceutical formulation, technology and engineering should be directed to our sister e-journal, AAPS PharmSciTech. The Journal is indexed by PubMed/Medline, Index Medicus, Institute of Scientific Information's Science Citation Index and Chem Abstracts.
Editor-in-Chief, Ho-Leung Fung, Ph.D., oversees an international editorial board of leading researchers in the pharmaceutical sciences. Dr. Fung is Professor of Pharmaceutical Sciences at the University at Buffalo, The State University of New York.
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About AAPS
American Association of Pharmaceutical Scientists
http://www.aaps.org/index.asp
AAPS Pharmaceutica is the web portal for the American Association of Pharmaceutical Scientists, a professional, scientific society of more than 12,000 members employed in academia, industry, government and other research institutes worldwide. Founded in 1986, AAPS provides a dynamic international forum for the exchange of knowledge among scientists to enhance their contributions to public health. AAPS offers timely scientific programs, on-going education, information resources, opportunities for networking, and professional development.
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About AAPS FDD (Formulation design and Development section)
http://www.aapspharmaceutica.com/inside/sections/fdd/index.asp 1
The Formulation Design & Development Section is comprised of members from many diverse backgrounds in industry, regulatory and academia who share a common interest in the area of formulation design, research and development - a multidisciplinary field drawing upon the physical, chemical, biological and engineering sciences. The primary goal of this section is to unite multiple scientific disciplines in a forum where they can share experimental results, consider new formulation and dosage form technologies, and discuss issues and concerns regarding the design and development of formulations/drug products for all dosage forms. This Section collaboratively interfaces with other sections which focus on pre-formulation, biopharmaceutics, formulation strategies, and manufacturing process optimization.
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Council of Scientific and Industrial Research, Govt. of India
http://rdpp.csir.res.in/csir_acsir/Home.aspx
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Department of Pharmaceutical Engineering, Institute of technology, Banaras Hindu University, Varanasi, India
http://itbhu.ac.in/phe/
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(Meenakshi Dhanawat)
Ms. Meenakshi Dhanawat, Senior Research Fellow, Department of Pharmaceutical Engineering, IT-BHU presented her research Paper on “Design, Synthesis and Evaluation of New Hetroaryl Compounds having 5HT1A/2A Receptor Affinity” in AAPS National Biotechnology Conference, held from 16-19 May 2010 at San Francisco, California, USA.
Financial assistance was given by DBT (Department of Biotechnology, Ministry of Science & Technology) and Banaras Hindu University. She also received travel award from the AAPS DDD section to attend the conference. Currently, she is pursuing PhD in the field of Anticonvulsants under the supervision Dr. S. K. Shrivastava, Associate Professor, Pharmaceutical Chemistry.
The paper presented at AAPS was a group work from the lab of Department of Pharmaceutical Engineering (http://itbhu.ac.in/phe/). It was a joint effort by Meenakshi Dhanawat, Nirupam Das (both research scholars) and Dr. S. K. Shrivastava.
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About authors:
*Meenakshi Dhanawat:
Research Scholar, Department of Pharmaceutical Engineering, IT-BHU
Email: mdanawat.rs.phe@itbhu.ac.in
* Nirupam Das:
Research Scholar, Department of Pharmaceutical Engineering, IT-BHU
Email: Nirupam.pharma@gmail.com |
*Dr. S. K. Shrivastava
Associate Professor, Department of Pharmaceutical Engineering, IT-BHU
Email: skshrivastava.phe@itbhu.ac.in
Background of research (by Meenakshi Dhanawat):
My research is contributed in the field of anticonvulsants in a layman language drug against epilepsy. Epilepsy is biomedical disturbances in which clusters of nerve cells, or neurons, in the brain sometimes signal abnormally that may remain localized (focal epilepsy) become widespread (generalized epilepsy). It is a global threat and therefore need attention of scientists to bring new molecules to fight against the developing resistance developed to existing drugs. Being effective drug should be safe also with this aim we are trying to synthesize compounds, which can target newly discovered 5HT1A/2A receptor. Serotonin or 5-Hydroxytryptamine (5-HT) is a monoamine neurotransmitter, biochemically derived from tryptophan that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. Specifically 5HT1A/2A is more concern to epilepsy therefore we have selected this one. In the initial phase of study we got satisfactory results and have plans to go to carry forward to next level as soon as we have finish all preliminary studies. It can be a good agent for protection against epilepsy in near future.
Educational Background of Meenakshi Dhanawat
2007-Present: Ph.D. (Pharmaceutical Chemistry), Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221005, U.P, India
2005-2007: M.S. (Pharm.) (Medicinal Chemistry), Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector-67, S.A.S. Nagar-160062
2000-2005: B. Pharm. Lachoo Memorial College of Science & Technology, Jodhpur, Rajasthan, India.
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http://www.aapsj.org/abstracts/NBC_2010/NBC10-000263.PDF
Design, Synthesis and Evaluation of New Hetroaryl Compounds having 5HT1A/2A Receptor
Affinity
M. Dhanawat1, N. Das1, S. K. Shrivastava1
1Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India
Title: Design, Synthesis and Evaluation of New Hetroaryl Compounds having 5HT1A/2A Receptor Affinity
Purpose:
The study was aimed to design, synthesize and evaluation of some heteroaryl compounds and screened by In-silico ADME study for anticonvulsant activity.
Methods:
Twenty-two derivatives were synthesized to evaluate anticonvulsant activity. The synthesis of title compounds has been realized in two steps (scheme: 1). In the first step N-3 alkylation of phenytoin was done by reacting phenytoin with 1-bromo-2-chloro-ethane (n=2) and 1-bromo-3-chloro- propane (n=3) respectively. In the second step these intermediate were converted into respective derivatives by reacting with 1-aryl-piperazine and aniline derivatives in DMF/DMSO according to the method reported by Zha et al.2004. All synthesized compounds were purified, analyzed and evaluated for anticonvulsant activity by using the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) screens. Their neurotoxicity was determined applying the rotarod test. In-silico ADME studies were also performed for preliminary screening. Ligands were built using Maestro 8.5 build panel and prepared by LigPrep 2.2 version v22208 (Schrödinger, LLC., USA) application that uses OPLS 2005 force field. The QikProp program was used to obtain the ADME properties of the analogues. The bestfit ligands were neutralized before being used by QikProp.
Results:
Structures of all the synthesized compounds were confirmed by spectral analysis: IR, 1 H and 13 C NMR, Mass spectroscopy. Reactions were optimized with different solvents and bases that yielded a compound good to moderate. In-silico ADME studies were also performed for preliminary screening. This also shows good to moderate results. Preliminary screening results indicated that the title compounds have pronounced anti-MES activity. A series of new hetroaryl derivatives of 5,5- dipheylhydrantoin showed Anticonvulsant activity. According to the rotarod test none of the compounds showed neurotoxicity at the applied dose. 1-aryl piperazine derivatives were found to have more active then aniline derivatives.
Conclusion:
Hetroaryl derivatives were successfully synthesized with good yield and screened compound showed anticonvulsant activity against phenytoin.
____________________________________
About AAPS Journal
About The AAPS Journal
The AAPS Journal (ISSN 1550-7416) is an online-only journal publishing peer-reviewed scholarly reviews, themed issues and research articles within the entire scope of the pharmaceutical sciences encompassed by the AAPS membership. The Journal particularly aims to foster the dissemination of scientific information presented at AAPS-sponsored meetings, workshops and symposia, through the publication of invited reviews in themed issues. Additionally, guest editors are invited to organize special themed issues on scientific subjects of current interest. Submission of uninvited expert reviews and research articles in all areas of pharmaceutical sciences are welcomed, although manuscripts focused on pharmaceutical formulation, technology and engineering should be directed to our sister e-journal, AAPS PharmSciTech. The Journal is indexed by PubMed/Medline, Index Medicus, Institute of Scientific Information's Science Citation Index and Chem Abstracts.
Editor-in-Chief, Ho-Leung Fung, Ph.D., oversees an international editorial board of leading researchers in the pharmaceutical sciences. Dr. Fung is Professor of Pharmaceutical Sciences at the University at Buffalo, The State University of New York.
_____________________________________
About AAPS
American Association of Pharmaceutical Scientists
http://www.aaps.org/index.asp
AAPS Pharmaceutica is the web portal for the American Association of Pharmaceutical Scientists, a professional, scientific society of more than 12,000 members employed in academia, industry, government and other research institutes worldwide. Founded in 1986, AAPS provides a dynamic international forum for the exchange of knowledge among scientists to enhance their contributions to public health. AAPS offers timely scientific programs, on-going education, information resources, opportunities for networking, and professional development.
__________________________________
About AAPS DDD (Drug design and Discovery section)
http://www.aaps.org/inside/sections/ddd/index.asp
1
Who We Are:
The DDD Section engages in all aspects of the design and discovery of molecular pharmaceutical entities, and fosters interactions at the interface between drug discovery and development. DDD provides leadership and a forum for interactions among scientists from academia, industry, and research institutions. The section invites and supports collaborative relationships with scientists in other disciplines within AAPS and other scientific and professional organizations whose efforts are directed toward the interface of drug design and discovery and drug development. The DDD Section is truly unique among scientific organizations serving the needs of medicinal and natural products chemists and scientists engaged in other emerging technologies and disciplines involved in drug development, including druggability, by providing a single organization for all members associated with pharmaceutical drug discovery and development.
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Department of Biotechnology, Ministry of Science & Technology, Govt. of India
http://dbtindia.nic.in/index.asp
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Department of Pharmaceutical Engineering, Institute of technology, Banaras Hindu University, Varanasi, India
http://itbhu.ac.in/phe/
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Institute of Technology, Banaras Hindu University
Varanasi 221005, UP