Day 1 :
- Drug Delivery Technologies
Session Introduction
Sherif Ashraf Fahmy
American University in Cairo ,Egypt
Title: Chitosan-Coated PLGA Nanoparticles Loaded with Peganum harmala Alkaloids with Promising Antibacterial and Wound Healing Activities
Biography:
Dr. Sherif Ashraf Fahmy his Ph. D. in Chemistry from the American University in Cairo in collaboration with the Department of Pharmaceutics & Biopharmaceutics, Faculty of Pharmacy, Philipps-Universität Marburg, Germany. He was selected as one of the first recipients of the prestigious fellowship offered by the Alfi Foundation for Ph.D. students. He has received several other awards, most notably, the Royal Society of Chemistry (RSC, UK) Travel Grant for Early Career Scientists in 2019, the Fulbright Scholarship at Ohio University (2019), USA. Dr. Fahmy has published several peer-reviewed articles in international journals and many abstracts at international conferences. He is a member of the Royal Society of Chemistry (MRSC) and the American Chemical Society (ACS). Also, he serves as a reviewer for many international journals. Dr. Fahmy is a full-time Assistant Professor of Chemistry and Head of the Nanomedicine & Phytochemicals research group at the University of Hertfordshire, Egypt Campus
Abstract:
Wound healing is a major healthcare concern, and complicated wounds may lead to severe outcomes such as septicemia and amputations. To date, management choices are limited, which warrants the search for new potent wound healing agents. Natural products loaded in poly (lactic-co-glycolic acid) (PLGA) coated with chitosan (CS) constitute a promising antibacterial wound healing formulation. In this work, harmala alkaloid-rich fraction (HARF) loaded into PLGA nanoparticles coated with chitosan (H/CS/PLGA NPs) were designed using the emulsion-solvent evaporation method. Optimization of the formulation variables (HARF: PLGA and CS: PLGA weight ratios, sonication time) was performed using the 33 Box–Behnken design (BBD). The optimal NPs were characterized using transmission electron microscopy (TEM) and Attenuated Total Reflection Fourier-Transformed Infrared Spectroscopy (ATR-FTIR). The prepared NPs had an average particle size of 202.27 ± 2.44 nm, a PDI of 0.23 ± 0.01, a zeta potential of 9.22 ± 0.94 mV, and an entrapment efficiency of 86.77 ± 4.18%. In vitro drug release experiments showed a biphasic pattern where an initial burst of 82.50 ± 0.20% took place in the first 2 h, which increased to 87.50 ± 0.50% over 72 h. The designed optimal H/CS/PLGA NPs exerted high antibacterial activity against Staphylococcus aureus and Escherichia coli (MIC of 0.125 and 0.06 mg/mL, respectively) compared to unloaded HARF (MIC of 0.50 mg/mL). The prepared nanoparticles were found to be biocompatible when tested on human skin fibroblasts. Moreover, the wound closure percentage after 24 h of applying H/CS/PLGA NPs was found to be 94.4 ± 8.0%, compared to free HARF and blank NPs (68.20 ± 5.10 and 50.50 ± 9.40%, respectively). In conclusion, the three components of the developed nanoformulation (PLGA, chitosan, and HARF) have synergistic antibacterial and wound healing properties for the management of infected wounds.
Zerihun Tesfaye Nigussie
Addis Ababa University,Ethiopia
Title: Screening Of Aloe otallensis Exudate and Its Effect on L .Donovani Paracite
Biography:
Abstract:
Tamrat Balla
School of Pharmacy Wolaita Sodo University, Ethiopia
Title: Optimization of Pregelatinized Taro Boloso-I Starch as a Direct Compression Tablet Excipient
Biography:
Tamrat Balcha has his expertise in Table Preparation, development of excipients such as tablet disintegrants and direct compression tablet filler-binders. His experience in the central composite design for optimization of formulation and process variables in the drug delivery systems is immense. He has more than 6 years of teaching experience in pharmaceutics.
Abstract:
Background. Tablets are still the most preferred means of drug delivery. The search for new and improved direct compression tablet excipients is an area of research focus. This is because the direct compression method overcomes the drawbacks of granulation methods of tablet production. It exempts several treatment steps associated with the granulation methods. The requirements for the powders to be directly compressible include flowability, low friction tendency, compressibility, and fast disintegration capacity. Taro Boloso-I is a new variety of Colocasia esculenta (L. Schott) yielding 67% more than a previously reported variety (Godare) in Ethiopia. This study is aimed at enhancing the flowability while keeping the compressibility and compactibility of the pregelatinized Taro Boloso-I starch. Methods. Central composite design was used for the optimization of two factors which were the temperature and duration of pregelatinization against 4 responses. The responses were angle of repose, Hausner’s ratio, Heckel’s yield pressure, and tablet breaking force. Results and Discussions. An increase in the temperature resulted in decrease in both the angle of repose and the Hausner ratio and that of time decreased angle of repose as well. The Heckel yield pressure was observed to increase with increasing levels of both temperature and time. The pregelatinized starch prepared by heating 15% slurry of Taro Boloso-I starch at the pregelatinization temperature of 66.22°C for 20 min showed desired flow property and compressibility. Conclusions. Pregelatinized Taro Boloso-I starch could be regarded as a potential direct compression excipient in terms of flowability, compressibility, and compactibility. The PGTBIS could perform better as filler and binder in direct compression tablets than the Starch 1500® in terms of compactibility.
- Routes of Drug Administration
Session Introduction
Lydia Ferenje
Ministry of Health, Ethiopia
Title: Rational Use Of Anti-Malarial Drugs On The Management Of Malaria Cases And The Rational Prescribing Practice Of Antimalarial, The Case Of Ethiopian Teaching Hospital: Retrospective Crossectional Study
Biography:
Abstract:
Background: Malaria is a major cause of morbidity and mortality in the developing countries. Appropriate use of recommended antimalarial drugs is vital in the effective management of malaria. Rational use of antimalarial drugs reduces the development of drug resistance and cost of therapy. Anti-malaria agents have been used for the management of malaria infections over the years in Ethiopia. However, not much is known about the quality of its use.
Objectives: To evaluate the rational use of anti-malarial Drugs on the Management of Malaria Cases and the Rational Prescribing Practice of Antimalarial in Mizan Tepi University hospital, south west Ethiopia.
Methodology: A 1-year retrospective cross-sectional study (chart review) was conducted from July1- to July30/2021. Charts (Data) of 125 patients were reviewed on socio-demographics, rational use of anti-malarial agents as per 2021, guidelines and outcomes.
Results and discussion: A total of 125 patients treated with the Antimalaria drug were reviewed. Of these, 65 (52%) were female. Ninety-one (72.8%) of the subjects belonged to 15 years and older age group. Laboratory test was requested for, 64(51.2%) patients. Forty-five patients were positive for malaria. Twenty-five patients had Plasmodium falciparum following Plasmodium vivax (n=18), and two patients had co-infection. Uncomplicated malaria cases were 15 (12%) whereas 9(7.2%) cases were severe malaria. Artemisinin – Lumefantrine was the most prescribed antimalarial drugs, 70(49.65%) following Artesunate and Chloroquine were, 36(25.53%) and 35(24.82%) respectively. Weight for those properly diagnosed and had severed malaria before Artesunate injection administered was recorded only for 3 (50%) patients. Seven of the patients have not taken single dose of Primaquine despite national malaria treatment guideline recommendation. Even though weight based was appropriate, more than two-third of the patients (82 (65.6 %)) were treated without weight measurement. Four of the patients had taken Primaquine daily for 14 days. Hemoglobin measurement with in the recommended days was not checked for those who were taking Primaquine.
Conclusion: Only 45 confirmed malaria cases among treated 125 patients. Treating patients with Antimalaria drugs irrespective of causative agent was common. Problem of adherence to malaria treatment guideline was observed. Intervention on irrational antimalarial drug use in MTUTH needs concern.
- Advanced Drug Delivery Systems
Session Introduction
Rajendran (Raj) Arunagiri
Global Pharma Segment Manager, Eastman, TN, USA
Title: New excipient to formulate poorly soluble APIs
Biography:
Rajendran (Raj) Arunagiri is the Global Pharma Segment Manager at Eastman. Raj has nearly a decade of experience in the pharma industry interfacing with the entire pharma value chain across the globe. Raj’s expertise is understanding global drug delivery trends. Raj has an Electrical Engineering degree from India and an MBA from USA.
Abstract:
One of the toughest challenges facing the drug development today is poor solubility of the API. It is estimated that 70%+ of the APIs in drug development pipeline are poorly soluble in water. There are several approaches to this problem with many requiring processes such as spray drying and hot melt extrusion, complex manufacturing processes. Through our presentation we would like to introduce a new tool to formulate poor water-soluble APIs without the need for spray drying or hot melt extrusion. Through this talk we would like to present our formulation studies with several poorly soluble API. Our dataset for the presentation will include mechanism of action, dissolution, stability, and bioavailability. The presentation will also highlight the formulations of two examples APIs (Aprepitant and Tacrolimus) for the case study. We will also demonstrate the safety of the new excipient and share recently approved reference drug. While not the main topic, we will also demonstrate how this new tool enables the formulation of long acting injectable without the need for any implants
- Drug repurposing to treat Viruses: COVID-19
Session Introduction
Alpana Bastikar
NSRT, Research Scientist, India
Title: Targeting SARS-COV2 Main Protease Using HTVS and Simulation Analysis: A Drug Repurposing Approach against COVID-19
Biography:
Alpana Bastikar is a computational chemist and bioinformatician in the field of computer aided drug design and bioinformatics industry. Highly well versed with all the licensed computational softwares and also having experience in preparing dossiers for Europe and other countries. She Is Diligent and resourceful professional with excellent analytical and communication skills. She is exceedingly motivated, Methodical and well organized in work culture. She Is a strong team player possessing skillful leadership potentials.
Abstract:
Coronavirus pandemic COVID 19 has caused a wide range of harm worldwide with its inception in December 2019 in Wuhan, China. To date there is no promising drug identified for the treatment of disease. In the view of this, scientists have elucidated X-ray structures of the proteins in SARS-COV2 virus. These can act as probable drug targets for the designing of drugs what is urgent need. One of the main proteins of the virus is its main protease M pro which is responsible for producing polyproteins of the virus. In this study we have used main protease as the target for drug design and repurposing for COVID-19. Two approaches were applied in order to develop a fast and effective treatment against the virus. The first approach was drug repurposing through in-silico docking analysis of existing FDA approved drugs and the second approach was high throughput screening of molecules from the ZINC database against main protease. Two docking protocols-a fast docking algorithm to screen the hits or lead molecules and simulation based molecular dynamics docking procedure to optimize the obtained hits were utilized. We could observe a definite scaffold based binding affinity against the main protease. These scaffolds were lutein, steroids, morphine and quinolone, CPT. Thiotepa was identified as the best docked molecule with highest binding affinity. Unique molecules like lutein, beta carotene, Buprenorphine etc were identified as promising hits which can be used as repurposed drugs against SARS-COV2. Also these scaffolds show unique pharmacophores that can be utilized to design potential novel leads against