Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4487
Nguyen Thanh Lam, Ngo Giao Thong, Tran Thi My Duyem, Bui Thi Thuong, Tran Thi Hai Yen
Abstract: Leuprolide acetate (LA) - a nonapeptide, used for the treatment of some hormone-depending diseases, is unstable and very susceptible to degradation in the aqueous media. Poly (lactic-co-glycolic) acid (PLGA) is a copolymer of lactide and glycolide, that has generated tremendous interest in pharmaceutics because of their excellent biocompatibility, biodegradability, and mechanical strength. PLGA is used for the preparation of biocompatible biodegradable extended-release microspheres. However, the PLGA undergoes hydrolytic degradation in an aqueous environment through cleavage of its backbone ester linkages. As a consequence, PLGA-based microspheres loaded with LA are usually lyophilized to ensure the stability of LA and PGLA and reduce agglomeration, sedimentation, and size change of microspheres during storage. The aim of this present study is to evaluate the influence of lyoprotectants namely mannitol, trehalose, lactose, and saccharose on the stability of LA and characteristics of PLGA-based microspheres loaded with LA upon lyophilization. DSC and FTIR were used to evaluate the biocompatibility of LA and lyoprotectants. The results showed that there was no incompatibility between the LA and lyoprotectants. Mannitol solution 1.25% was used in freeze-drying PLGA-based microspheres loaded with LA. The obtained lyophilized microspheres had a good appearance and low moisture. Lyophilized microspheres after reconstitution had no significant change in drug content, size, and size distribution in comparison to that before freeze-drying. Keywords: Leuprolide acetate, PGLA, lyophilized, stability, biodegradable microspheres.
{"title":"Investigation of Lyophilized Microspheres Loaded with Leuprolide Acetate","authors":"Nguyen Thanh Lam, Ngo Giao Thong, Tran Thi My Duyem, Bui Thi Thuong, Tran Thi Hai Yen","doi":"10.25073/2588-1132/vnumps.4487","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4487","url":null,"abstract":"Abstract: Leuprolide acetate (LA) - a nonapeptide, used for the treatment of some hormone-depending diseases, is unstable and very susceptible to degradation in the aqueous media. Poly (lactic-co-glycolic) acid (PLGA) is a copolymer of lactide and glycolide, that has generated tremendous interest in pharmaceutics because of their excellent biocompatibility, biodegradability, and mechanical strength. PLGA is used for the preparation of biocompatible biodegradable extended-release microspheres. However, the PLGA undergoes hydrolytic degradation in an aqueous environment through cleavage of its backbone ester linkages. As a consequence, PLGA-based microspheres loaded with LA are usually lyophilized to ensure the stability of LA and PGLA and reduce agglomeration, sedimentation, and size change of microspheres during storage. The aim of this present study is to evaluate the influence of lyoprotectants namely mannitol, trehalose, lactose, and saccharose on the stability of LA and characteristics of PLGA-based microspheres loaded with LA upon lyophilization. DSC and FTIR were used to evaluate the biocompatibility of LA and lyoprotectants. The results showed that there was no incompatibility between the LA and lyoprotectants. Mannitol solution 1.25% was used in freeze-drying PLGA-based microspheres loaded with LA. The obtained lyophilized microspheres had a good appearance and low moisture. Lyophilized microspheres after reconstitution had no significant change in drug content, size, and size distribution in comparison to that before freeze-drying. \u0000Keywords: Leuprolide acetate, PGLA, lyophilized, stability, biodegradable microspheres. \u0000 \u0000 ","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"60 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83006189","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract: Implementation of in vivo bioequivalence study is a growing trend in the pharmaceutical industry in Vietnam and over the world. These studies are required in order to demonstrate whether a generic drug is a bioequivalence to an innovator’s drug or to an original brand name drug. At present, there are 26 active ingredients that have to provide in vivo bioequivalence study report for drug registration in Vietnam. In the next few years, this number will gradually increase. Therefore, the government should introduce promotion, development, and preferential policies for enterprises to invest in these ingredients. This paper aims to provide general guidelines on regulations of in vivo bioequivalence studies for pharmaceutical enterprises in Vietnam and support the initial implementation of these studies in practice. Keywords: Bioequivalence, BABE, BE, Regulations.
{"title":"In Vivo Bioequivalence Study of Drug: An Analysis of Related Regulations in Current Pharmaceutical Legislation in Vietnam","authors":"Tang Quoc Hung, Nguyen Thi Thanh Hai, Tran Bich Ngoc","doi":"10.25073/2588-1132/vnumps.4474","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4474","url":null,"abstract":"Abstract: Implementation of in vivo bioequivalence study is a growing trend in the pharmaceutical industry in Vietnam and over the world. These studies are required in order to demonstrate whether a generic drug is a bioequivalence to an innovator’s drug or to an original brand name drug. At present, there are 26 active ingredients that have to provide in vivo bioequivalence study report for drug registration in Vietnam. In the next few years, this number will gradually increase. Therefore, the government should introduce promotion, development, and preferential policies for enterprises to invest in these ingredients. This paper aims to provide general guidelines on regulations of in vivo bioequivalence studies for pharmaceutical enterprises in Vietnam and support the initial implementation of these studies in practice. \u0000Keywords: Bioequivalence, BABE, BE, Regulations.","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74795244","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4351
Doan Van Ngoc, Tran Anh Tuan, Hoang Dinh Au
Abstract: A study of 135 cases without cerebral vascular malformations who were scan MSCT of cerebral arteries at Bach Mai hospital during the period from January 2019 to December 2019. Result: mean diameter of cerebral artery segments: left and right A1 segments: 2.28 ± 0.47 and 2.19 ± 0.53 mm; AcomA: 1.71 ± 0.68 mm; left and right M1 segments: 2.82 ± 0.46 mm and 2.8 ± 0.49 mm; left and right PcomA: 1.62 ± 0.5 mm and 1.67 ± 0.48 mm; left and right P1 segments: 2.22 ± 0.49 mm and 2.22 ± 0.56 mm; left and right P2 segments: 2.32 ± 0.38 mm and 2.35 ± 0.36 mm; BA: 3.41 ± 0.69 mm. The diameters of the cerebral arteries were similar in both sexes, with no difference on the right and left sides of the ring of Willis. The diameter of the edges of the Willis circle varied from aplastic and hypoplastic, which was mainly seen in the AcomA, PcomA, the A1 segment of the anterior cerebral artery, and P1 of the posterior cerebral artery. The transformations of the Willis ring included 17 forms, of which four simple transformations of the anterior part, four simple transformations of the posterior part, and nine combined transformations between the anterior and posterior parts. Mainly found aplasia or hypoplasia of the AcomA 14.1% and the PcomA 12.6%. Conclusion: the index of normalization of the segments of the Willis polygon and its variant forms contributed to bolder intervention planning in cerebrovascular disease treatment. Keywords: Circle of Willis, Cerebral arteries, MSCT.
{"title":"The Features of the Circle of Willis on Multislice Computed Tomography in Humans Without Cerebral Vascular Malformations","authors":"Doan Van Ngoc, Tran Anh Tuan, Hoang Dinh Au","doi":"10.25073/2588-1132/vnumps.4351","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4351","url":null,"abstract":"Abstract: A study of 135 cases without cerebral vascular malformations who were scan MSCT of cerebral arteries at Bach Mai hospital during the period from January 2019 to December 2019. Result: mean diameter of cerebral artery segments: left and right A1 segments: 2.28 ± 0.47 and 2.19 ± 0.53 mm; AcomA: 1.71 ± 0.68 mm; left and right M1 segments: 2.82 ± 0.46 mm and 2.8 ± 0.49 mm; left and right PcomA: 1.62 ± 0.5 mm and 1.67 ± 0.48 mm; left and right P1 segments: 2.22 ± 0.49 mm and 2.22 ± 0.56 mm; left and right P2 segments: 2.32 ± 0.38 mm and 2.35 ± 0.36 mm; BA: 3.41 ± 0.69 mm. The diameters of the cerebral arteries were similar in both sexes, with no difference on the right and left sides of the ring of Willis. The diameter of the edges of the Willis circle varied from aplastic and hypoplastic, which was mainly seen in the AcomA, PcomA, the A1 segment of the anterior cerebral artery, and P1 of the posterior cerebral artery. The transformations of the Willis ring included 17 forms, of which four simple transformations of the anterior part, four simple transformations of the posterior part, and nine combined transformations between the anterior and posterior parts. Mainly found aplasia or hypoplasia of the AcomA 14.1% and the PcomA 12.6%. Conclusion: the index of normalization of the segments of the Willis polygon and its variant forms contributed to bolder intervention planning in cerebrovascular disease treatment. \u0000Keywords: Circle of Willis, Cerebral arteries, MSCT.","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86662025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4433
Abstract: This study aims to describe the clinical and subclinical characteristics of patients with castration-resistant prostate cancer (CRPC). The retrospective study was conducted on 46 patients with CRPC in Huu Nghi Hospital. The results indicated that the main clinical symptoms were bone pain (63.0%), hematuria (34.0%), and lower urinary tract symptoms (32.6%). The highest and lowest PSA concentrations were 611.3 ng/mL and 0.01 ng/mL, respectively. The most common sites of metastasis were bone (82.6%), lymph node (50.0%), and lung (19.6%). These patients were all at the late stage, so most of them had symptoms of metastasis and high PSA. Keywords: Prostate cancer, castration-resistant, clinical characteristics, subclinical characteristics.
{"title":"Some Clinical and Subclinical Characteristics of Patients with Castration-resistant Prostate Cancer in Huu Nghi Hospital","authors":"","doi":"10.25073/2588-1132/vnumps.4433","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4433","url":null,"abstract":"Abstract: This study aims to describe the clinical and subclinical characteristics of patients with castration-resistant prostate cancer (CRPC). The retrospective study was conducted on 46 patients with CRPC in Huu Nghi Hospital. The results indicated that the main clinical symptoms were bone pain (63.0%), hematuria (34.0%), and lower urinary tract symptoms (32.6%). The highest and lowest PSA concentrations were 611.3 ng/mL and 0.01 ng/mL, respectively. The most common sites of metastasis were bone (82.6%), lymph node (50.0%), and lung (19.6%). These patients were all at the late stage, so most of them had symptoms of metastasis and high PSA. \u0000Keywords: Prostate cancer, castration-resistant, clinical characteristics, subclinical characteristics. \u0000 \u0000 \u0000 ","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87470184","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4387
Nguyen Thi Hai Yen, Phung The Hiep, Nguyen Thi My Dung, Le Ngoc Danh, Thai Hue Ngan, Le Dang Tu Nguyen
Abstract: Drug procurement bidding has always been under the government’s particular concern to assure drug quality, stabilize drug costs, and enhance the use of domestic drugs. A retrospective study analyzes data from the drug procurement results in Vietnam from 2013 to 2020 based on the results reported to the Drug Administration of Vietnam. The rate of drugs selected through the bidding process in Hanoi and HCMC accounted for the highest proportion in the country with 17.5% and 14.3%, respectively. The number of selected drugs with domestic origins had seen a gradual increase over the years with 4545 drugs during 2020, which was 2.2 times higher than that of 2013 (2079 drugs). Generic drugs in group 3 with domestic origins comprised the highest proportion of both quantity and value compared to drugs in other groups. Antiparasitic drugs and anti-infectives had the highest value rates among pharmacological groups with over 20%. During the research period, the costs of selected drugs tended to witness a decreasing trend, accounting for 60% of drugs. Only 9% of the drugs had their values remain unchanged, and the other 31% saw an increase in these values. State bidding procurement policies are making positive effects in lowering drug costs and encouraging domestic drug use. However, the value rate of domestic drugs is still lower than that of imported ones. It is necessary for domestic pharmaceutical enterprises to invest in developing factories, actively find domestic ingredient sources, and focus on specific medications in great demand. Keywords: Drug bidding, drug price, generic bidding package, original brand name bidding package, period of 2013-2020, Vietnam.
{"title":"Analysis of Drug Procurement Results in Vietnam from 2013 to 2020","authors":"Nguyen Thi Hai Yen, Phung The Hiep, Nguyen Thi My Dung, Le Ngoc Danh, Thai Hue Ngan, Le Dang Tu Nguyen","doi":"10.25073/2588-1132/vnumps.4387","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4387","url":null,"abstract":"Abstract: Drug procurement bidding has always been under the government’s particular concern to assure drug quality, stabilize drug costs, and enhance the use of domestic drugs. A retrospective study analyzes data from the drug procurement results in Vietnam from 2013 to 2020 based on the results reported to the Drug Administration of Vietnam. The rate of drugs selected through the bidding process in Hanoi and HCMC accounted for the highest proportion in the country with 17.5% and 14.3%, respectively. The number of selected drugs with domestic origins had seen a gradual increase over the years with 4545 drugs during 2020, which was 2.2 times higher than that of 2013 (2079 drugs). Generic drugs in group 3 with domestic origins comprised the highest proportion of both quantity and value compared to drugs in other groups. Antiparasitic drugs and anti-infectives had the highest value rates among pharmacological groups with over 20%. During the research period, the costs of selected drugs tended to witness a decreasing trend, accounting for 60% of drugs. Only 9% of the drugs had their values remain unchanged, and the other 31% saw an increase in these values. State bidding procurement policies are making positive effects in lowering drug costs and encouraging domestic drug use. However, the value rate of domestic drugs is still lower than that of imported ones. It is necessary for domestic pharmaceutical enterprises to invest in developing factories, actively find domestic ingredient sources, and focus on specific medications in great demand. \u0000Keywords: Drug bidding, drug price, generic bidding package, original brand name bidding package, period of 2013-2020, Vietnam. \u0000 \u0000 ","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"65 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74102715","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4405
Nguyen Thi Lien, Nguyen Thi Hang
Abstract: Ich tri Hadiphar capsules used for dementia treatment were evaluated for acute and repeated dose toxicities in mice and rabbits, respectively. The acute toxicity results indicated that LD50 of Ich tri Hadiphar capsules in mice according to the method of Behrens is greater than 30 g/kg body weight. In the repeated dose toxicity study, rabbits were administrated Ich tri Hadiphar with doses of 186.5 and 560.0 mg/kg/day for 28 days (equivalent to the dose used on humans and the dose of 3 times more than one used on humans). Blood samples were taken on day 0, day 14, and day 28 of the experiment for hematological and biochemical analysis. Liver and kidney samples were taken on day 28 for histopathological determinations. The repeated dose toxicity results revealed that there were no significant differences in hematological and serum biochemical values between control and treatment animals. Furthermore, no histopathological changes in the liver and kidney of rabbits treated with Ich tri Hadiphar capsules were observed. Keywords: Acute toxicity, repeated dose toxicity, Ich tri Hadiphar.
摘要:本研究分别在小鼠和家兔实验中评价了用于治疗痴呆的Ich tri Hadiphar胶囊的急性毒性和重复剂量毒性。急性毒性实验结果表明,按Behrens法给药的小鼠LD50大于30 g/kg体重。在重复给药毒性研究中,家兔以186.5和560.0 mg/kg/天的剂量连续28天(相当于人用剂量,是人用剂量的3倍以上)给予Ich trihadiphar。于实验第0天、第14天、第28天采血,进行血液学和生化分析。第28天取肝、肾标本进行组织病理学检查。重复剂量毒性试验结果显示,对照动物和处理动物的血液学和血清生化指标无显著差异。此外,Ich tri Hadiphar胶囊对家兔肝脏和肾脏未见组织病理学改变。关键词:急性毒性,重复剂量毒性,Ich tri Hadiphar。
{"title":"Acute and Repeated Dose 28-day Oral Toxicity Studies of Ich Tri Hadiphar Capsules","authors":"Nguyen Thi Lien, Nguyen Thi Hang","doi":"10.25073/2588-1132/vnumps.4405","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4405","url":null,"abstract":"Abstract: Ich tri Hadiphar capsules used for dementia treatment were evaluated for acute and repeated dose toxicities in mice and rabbits, respectively. The acute toxicity results indicated that LD50 of Ich tri Hadiphar capsules in mice according to the method of Behrens is greater than 30 g/kg body weight. In the repeated dose toxicity study, rabbits were administrated Ich tri Hadiphar with doses of 186.5 and 560.0 mg/kg/day for 28 days (equivalent to the dose used on humans and the dose of 3 times more than one used on humans). Blood samples were taken on day 0, day 14, and day 28 of the experiment for hematological and biochemical analysis. Liver and kidney samples were taken on day 28 for histopathological determinations. The repeated dose toxicity results revealed that there were no significant differences in hematological and serum biochemical values between control and treatment animals. Furthermore, no histopathological changes in the liver and kidney of rabbits treated with Ich tri Hadiphar capsules were observed. \u0000Keywords: Acute toxicity, repeated dose toxicity, Ich tri Hadiphar. \u0000 \u0000 \u0000 ","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86508348","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4409
Phan Hong Minh, Mai Phuong Thanh, Tran Thi Thu Trang, Ho My Dung
Abstract: Jasminum subtriplinerve Blume Oleaceae is a herbal medicine widely used for weight loss and milk gland stimulation. Extract product has been generally used but has not much scientific evidence about its safety and effects. This study aimed to evaluate the semi-chronic toxicity and lipid-lowering effects of Jasminum subtriplinerve Blume leaf extract. The study was performed on Wistar rats and Swiss mice. For semi-chronic toxicity, extracts at doses of 18 mg/kg/day and 54 mg/kg/day showed their safety after 90 days of continuous oral administration in Wistar rats. There was no effect on body weight, hematopoietic parameters, hepatocellular destruction, or liver and kidney function in experimental rats. For the lipid-lowering effect, the extracts at 36 mg/kg/day and 108 mg/kg/day showed a marked decrease in the blood lipid indexes (total cholesterol, triglycerides, non-HDL-C) after 7 days of dosing in Swiss mice on an endogenous dyslipidemic model induced by Poloxamer-407. Keywords: Jasminum subtriplinerve Blume Oleaceae, lipid-lowering, dyslipidemia, semi-chronic toxicity.
{"title":"Assessment of Semi-chronic Toxicity and Lipid-lowering Effect of Jasminum subtriplinerve Blume Oleaceae Extract","authors":"Phan Hong Minh, Mai Phuong Thanh, Tran Thi Thu Trang, Ho My Dung","doi":"10.25073/2588-1132/vnumps.4409","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4409","url":null,"abstract":"Abstract: Jasminum subtriplinerve Blume Oleaceae is a herbal medicine widely used for weight loss and milk gland stimulation. Extract product has been generally used but has not much scientific evidence about its safety and effects. This study aimed to evaluate the semi-chronic toxicity and lipid-lowering effects of Jasminum subtriplinerve Blume leaf extract. The study was performed on Wistar rats and Swiss mice. For semi-chronic toxicity, extracts at doses of 18 mg/kg/day and 54 mg/kg/day showed their safety after 90 days of continuous oral administration in Wistar rats. There was no effect on body weight, hematopoietic parameters, hepatocellular destruction, or liver and kidney function in experimental rats. For the lipid-lowering effect, the extracts at 36 mg/kg/day and 108 mg/kg/day showed a marked decrease in the blood lipid indexes (total cholesterol, triglycerides, non-HDL-C) after 7 days of dosing in Swiss mice on an endogenous dyslipidemic model induced by Poloxamer-407. \u0000Keywords: Jasminum subtriplinerve Blume Oleaceae, lipid-lowering, dyslipidemia, semi-chronic toxicity. \u0000 ","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87299672","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4489
Bui Thi Phuong Hai, Trinh Thi Kim Anh, Tran Thi Khanh Huyen, Luong Xuan Huy, Dang Thi Ngan, Bui Thi Thuong, N. Van Khanh, Nguyen Thi Thanh Hai, Nguyen Thi Thanh Binh
Abstract: Exploring the potential of natural bioactive peptides is becoming more and more important for new drug discovery. First isolated from the European wasp Vespa crabro, the antimicrobial peptide Mastoparan C was found in higher content than many other molecules in the Mastoparan family. In addition to the mast cell degranulation that is similar to some components in insect venom, this compound possesses remarkable biological activities such as broad-spectrum antibacterial and antifungal, inhibiting the proliferation of many human cancer cell lines. However, unfortunately, Mastoparan C has the notable side effect of causing mammalian hemolysis. By investigating its structure-activity relationships, this review pointed out some suggestions to overcome the disadvantages of this potential peptide and thereby support further in-depth study in the drug discovery field. Keywords: Mastoparan C, antimicrobial peptide, biological activity, structure-activity relationships.
{"title":"Potentialities of Antimicrobial Peptide Mastoparan C Isolated the European Hornet Vespa Crabro in Drug Discovery","authors":"Bui Thi Phuong Hai, Trinh Thi Kim Anh, Tran Thi Khanh Huyen, Luong Xuan Huy, Dang Thi Ngan, Bui Thi Thuong, N. Van Khanh, Nguyen Thi Thanh Hai, Nguyen Thi Thanh Binh","doi":"10.25073/2588-1132/vnumps.4489","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4489","url":null,"abstract":"Abstract: Exploring the potential of natural bioactive peptides is becoming more and more important for new drug discovery. First isolated from the European wasp Vespa crabro, the antimicrobial peptide Mastoparan C was found in higher content than many other molecules in the Mastoparan family. In addition to the mast cell degranulation that is similar to some components in insect venom, this compound possesses remarkable biological activities such as broad-spectrum antibacterial and antifungal, inhibiting the proliferation of many human cancer cell lines. However, unfortunately, Mastoparan C has the notable side effect of causing mammalian hemolysis. By investigating its structure-activity relationships, this review pointed out some suggestions to overcome the disadvantages of this potential peptide and thereby support further in-depth study in the drug discovery field. \u0000Keywords: Mastoparan C, antimicrobial peptide, biological activity, structure-activity relationships.","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"12 9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77896791","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4488
Vu Thi Thu Giang, Pham Thuy Hanh, Nguyen Van Lam
Abstract: Gynostemma pentaphyllum (Thunb.) Makino is a rich source of the herb in Vietnam. The gypenosides in this herb are triterpenoid saponins that have been shown to have moisturizing, antioxidant, and anti-aging effects on the skin. However, gypenosides are hydrophilic and have a large molecular weight with a bulk molecular structure which prevents them from penetrating and absorbing into the skin. To apply the natural active ingredients from herbs into skin care cosmetics, this research developed self-nano-emulsifying drug delivery systems (SNEDDS) containing Gynostemma pentaphyllum dry extract and applied them to emulgel skin care cosmetics. Prepared SNEDDS could self-emulsify in the water to form nanoemulsions with dispersed droplet sizes less than 20 nm with PDI < 0.3. The proportion of saponin entrapped in the oil droplets of nano emulsification was more than 90%. When combined with emulgel excipients, the obtained cosmetic products had nano-sized dispersed droplets less than 200 nm with uniform droplet size distribution, which are promising for application when further research is carried out. Keywords: Self-nano-emulsifying Drug Delivery System (SNEDDS), Gymnostemma pentaphyllum dry extract, cosmetic, emulgel, nano-emulsion.
{"title":"Research on the Preparation of Self-nano-emulsifying Drug Delivery System Containing Gynostemma pentaphyllum Dry Extract for Application in Skin Care Cosmetics","authors":"Vu Thi Thu Giang, Pham Thuy Hanh, Nguyen Van Lam","doi":"10.25073/2588-1132/vnumps.4488","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4488","url":null,"abstract":"Abstract: Gynostemma pentaphyllum (Thunb.) Makino is a rich source of the herb in Vietnam. The gypenosides in this herb are triterpenoid saponins that have been shown to have moisturizing, antioxidant, and anti-aging effects on the skin. However, gypenosides are hydrophilic and have a large molecular weight with a bulk molecular structure which prevents them from penetrating and absorbing into the skin. To apply the natural active ingredients from herbs into skin care cosmetics, this research developed self-nano-emulsifying drug delivery systems (SNEDDS) containing Gynostemma pentaphyllum dry extract and applied them to emulgel skin care cosmetics. Prepared SNEDDS could self-emulsify in the water to form nanoemulsions with dispersed droplet sizes less than 20 nm with PDI < 0.3. The proportion of saponin entrapped in the oil droplets of nano emulsification was more than 90%. When combined with emulgel excipients, the obtained cosmetic products had nano-sized dispersed droplets less than 200 nm with uniform droplet size distribution, which are promising for application when further research is carried out. \u0000Keywords: Self-nano-emulsifying Drug Delivery System (SNEDDS), Gymnostemma pentaphyllum dry extract, cosmetic, emulgel, nano-emulsion. \u0000 \u0000 \u0000 ","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88642875","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-03-25DOI: 10.25073/2588-1132/vnumps.4412
Ly Cong Thanh
Abstract: Anti-influenza-A drugs targeting viral neuraminidase have been in use for two decades. In this study, the quantitative structure-activity relationships (QSAR) of oseltamivir derivatives as influenza neuraminidase (IN) inhibitors have been explored using the Monte Carlo method based on the target function involving the index of the ideality of correlation. Three best-obtained models showed appropriate performance with R2 values of training and test sets ranging from 0.71 to 0.86, respectively. Based on the structural information extracted from the models, new inhibitors were designed and predicted for IN activities. Finally, protein docking was applied to confirm their target binding ability. Keyword: Anti-influenza A; neuramidase inhibitor; drug design; QSAR; docking.
{"title":"Towards Developing Quantitative Structure-activity Relationship Models for the Design of Novel Influenza A Inhibitors Targeting Neuraminidase","authors":"Ly Cong Thanh","doi":"10.25073/2588-1132/vnumps.4412","DOIUrl":"https://doi.org/10.25073/2588-1132/vnumps.4412","url":null,"abstract":"Abstract: Anti-influenza-A drugs targeting viral neuraminidase have been in use for two decades. In this study, the quantitative structure-activity relationships (QSAR) of oseltamivir derivatives as influenza neuraminidase (IN) inhibitors have been explored using the Monte Carlo method based on the target function involving the index of the ideality of correlation. Three best-obtained models showed appropriate performance with R2 values of training and test sets ranging from 0.71 to 0.86, respectively. Based on the structural information extracted from the models, new inhibitors were designed and predicted for IN activities. Finally, protein docking was applied to confirm their target binding ability. \u0000Keyword: Anti-influenza A; neuramidase inhibitor; drug design; QSAR; docking. \u0000 \u0000 ","PeriodicalId":23520,"journal":{"name":"VNU Journal of Science: Medical and Pharmaceutical Sciences","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81853356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}