Introduction: The anti-hypertensive drug Olmesartan Medoxomil (OLM), a BCS II drug, works by inhibiting the action of angiotensin II on AT1 receptors. Objectives: The purpose of the study was to enhance solubility and stability by altering crystalline form, which reduces cost and dose burden of the pharmaceutical industry. In the current study, OLM formulation was prepared by using a full 3 level 2 factorial design with chitosan and neusiline as independent factors. Materials and Methods: Chitosan, a hydrophilic and stabilizing polymer, was used to enhance solubility and stability with the help of neusiline as a surfactant. Formulation was prepare using microwave-assisted ball milled technology. Results and Discussion: In comparison to the pure drug, phase solubility study shows the ternary mixture's saturation solubility was around 12 times higher. Physical interaction between polymer and OLM was confirmed from the FTIR study, DSC graph, SEM surface morphological study and NMR study. The drug's altered crystalline form has been confirmed by XRD, which could alter its solubility and rate of dissolution. The optimized batch obtained from factorial design was used for electrically operated ball milling. This demonstrated a notable improvement in the solubility, stability, and dissolving rate. Conclusion: As a result, using chitosan with a microwave assisted ball milling process can be a novel breakthrough in enhancing the bioavailability of any BSC II medicines.
{"title":"Preparation and Optimization of Microwave-Assisted Ball-Milled Olmesartan Medoxomil with Chitosan Using Full 32 Factorial Design","authors":"Atul Shivaji Gurav, A. Kulkarni","doi":"10.5530/ijper.57.3s.64","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.64","url":null,"abstract":"Introduction: The anti-hypertensive drug Olmesartan Medoxomil (OLM), a BCS II drug, works by inhibiting the action of angiotensin II on AT1 receptors. Objectives: The purpose of the study was to enhance solubility and stability by altering crystalline form, which reduces cost and dose burden of the pharmaceutical industry. In the current study, OLM formulation was prepared by using a full 3 level 2 factorial design with chitosan and neusiline as independent factors. Materials and Methods: Chitosan, a hydrophilic and stabilizing polymer, was used to enhance solubility and stability with the help of neusiline as a surfactant. Formulation was prepare using microwave-assisted ball milled technology. Results and Discussion: In comparison to the pure drug, phase solubility study shows the ternary mixture's saturation solubility was around 12 times higher. Physical interaction between polymer and OLM was confirmed from the FTIR study, DSC graph, SEM surface morphological study and NMR study. The drug's altered crystalline form has been confirmed by XRD, which could alter its solubility and rate of dissolution. The optimized batch obtained from factorial design was used for electrically operated ball milling. This demonstrated a notable improvement in the solubility, stability, and dissolving rate. Conclusion: As a result, using chitosan with a microwave assisted ball milling process can be a novel breakthrough in enhancing the bioavailability of any BSC II medicines.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44801396","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract: Background: Natural biopolymers or hydrogels that are biodegradable and safe from biological point of view along with their capability to retain active principle within their network thus prolonging the release. The present work was undertaken to explore the potential of mucilage from mature seeds of Chia (Salvia hispanica) to sustain the release of water-soluble drugs. Losartan potassium was used as a model to prepare the gelispheres. Materials and Methods: The mucilage was isolated and their physicochemical properties like viscosity, phytoconstituent, FTIR, hydration index were studied. Gelispheres loaded with active drug Losartan Potassium (LP) were prepared using sodium alginate, pectin and CSM in various ratios by polyelectrolyte complexation (Ionic Gelation) method. Micrometric properties, surface contour analysis, ex vivo mucoadhesion study, in vitro drug release study, compatibility, XRD, stability study, statistical analysis was carried out on the prepared gelispheres. Results: The isolated mucilage of mature Chia (Salvia hispanica) seeds possesses immense properties like viscosity modification capacity, consistency, excellent hydration and mucoadhesive nature that can be explored for developing active principal delivery devices. Conclusion: The developed drug loaded gelispheres exhibited good mucoadhesion which enabled sustaining the release of drug for prolonged duration advocating the use of mucilage to design a twice daily losartan potassium sustain release system for management of hypertension. Keywords: Chia seed mucilage, Gelisphere, Mucoadhesion, Losartan potassium, Ionic gelation.
{"title":"Isolation and Functioning Investigation of Salvia hispanica Seed Mucilage as A Potential Sustained Release Carrier for Water Soluble Drug","authors":"Dibya Sundar Panda, Madhusmruti Khandai","doi":"10.5530/ijper.57.3s.82","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.82","url":null,"abstract":"Abstract: Background: Natural biopolymers or hydrogels that are biodegradable and safe from biological point of view along with their capability to retain active principle within their network thus prolonging the release. The present work was undertaken to explore the potential of mucilage from mature seeds of Chia (Salvia hispanica) to sustain the release of water-soluble drugs. Losartan potassium was used as a model to prepare the gelispheres. Materials and Methods: The mucilage was isolated and their physicochemical properties like viscosity, phytoconstituent, FTIR, hydration index were studied. Gelispheres loaded with active drug Losartan Potassium (LP) were prepared using sodium alginate, pectin and CSM in various ratios by polyelectrolyte complexation (Ionic Gelation) method. Micrometric properties, surface contour analysis, ex vivo mucoadhesion study, in vitro drug release study, compatibility, XRD, stability study, statistical analysis was carried out on the prepared gelispheres. Results: The isolated mucilage of mature Chia (Salvia hispanica) seeds possesses immense properties like viscosity modification capacity, consistency, excellent hydration and mucoadhesive nature that can be explored for developing active principal delivery devices. Conclusion: The developed drug loaded gelispheres exhibited good mucoadhesion which enabled sustaining the release of drug for prolonged duration advocating the use of mucilage to design a twice daily losartan potassium sustain release system for management of hypertension. Keywords: Chia seed mucilage, Gelisphere, Mucoadhesion, Losartan potassium, Ionic gelation.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"15 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135619915","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract: Background: Folk medicinal knowledge of plants is vital in primary health care management system, predominantly in rural and remote areas. Managing cuts and wounds continues to be a significant healthcare issue, and it becomes even more critical when left untreated or improperly treated. The objective of this study is to carry out a survey on the use of medicinal plants for treating cuts and wounds in the village of Kailashpur in Assam. Materials and Methods: The information was collected through a semi-structured questionnaire from 30 informants in Kailashpur, Assam, India. Quantitative analysis of these data to find Use Value (UV), Frequency of Citation (FC), Relative Frequency of Citation (RFC), Family Use Value (FUV), Consensus Index (CI), Rehman's Similarity Index (RSI) and Jaccard Index (JI) also completed. Results: The present study documented 45 medicinal plant species belonging to 30 families and their mode of application. Compositae (5 species), Orchidaceae (4 species) and Leguminosae (3 species) were dominant families. Leaves were the most frequently used plant part (PPV 0.50). Curcuma longa and Ocimum tenuiflorum (UV 0.33) were the species most commonly used by the local people. Highest FC was calculated for Ageratum conyzoids (5.27), followed by Tagetes erecta (4.51). JI and RSI indicated that plant species reported in our study were more similar to the Tezpur region of Assam, India. Conclusion: The findings emphasize the significance of specific plant species in the treatment of cuts and wounds, and suggest that further scientific investigation can be pursued to discover potential therapeutics. Keywords: Ethnomedicinal survey, Kailashpur village, Medicinal plants, Cuts, Wounds.
{"title":"Ethnobotanical Study of Medicinal Plants Used Traditionally for Managing Cuts and Wounds by the Rural People of Kailashpur, Assam, India","authors":"Pal Gogoi, Saikat Sen","doi":"10.5530/ijper.57.3s.77","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.77","url":null,"abstract":"Abstract: Background: Folk medicinal knowledge of plants is vital in primary health care management system, predominantly in rural and remote areas. Managing cuts and wounds continues to be a significant healthcare issue, and it becomes even more critical when left untreated or improperly treated. The objective of this study is to carry out a survey on the use of medicinal plants for treating cuts and wounds in the village of Kailashpur in Assam. Materials and Methods: The information was collected through a semi-structured questionnaire from 30 informants in Kailashpur, Assam, India. Quantitative analysis of these data to find Use Value (UV), Frequency of Citation (FC), Relative Frequency of Citation (RFC), Family Use Value (FUV), Consensus Index (CI), Rehman's Similarity Index (RSI) and Jaccard Index (JI) also completed. Results: The present study documented 45 medicinal plant species belonging to 30 families and their mode of application. Compositae (5 species), Orchidaceae (4 species) and Leguminosae (3 species) were dominant families. Leaves were the most frequently used plant part (PPV 0.50). Curcuma longa and Ocimum tenuiflorum (UV 0.33) were the species most commonly used by the local people. Highest FC was calculated for Ageratum conyzoids (5.27), followed by Tagetes erecta (4.51). JI and RSI indicated that plant species reported in our study were more similar to the Tezpur region of Assam, India. Conclusion: The findings emphasize the significance of specific plant species in the treatment of cuts and wounds, and suggest that further scientific investigation can be pursued to discover potential therapeutics. Keywords: Ethnomedicinal survey, Kailashpur village, Medicinal plants, Cuts, Wounds.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":"11 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135619916","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
D. Kavitha, R. Padmini, M. Dhanaraju, C. Gopi, D. Thiyagarajan, Alekkhya Veeramaneni
Background: Syringodium isoetifolium seagrass has bioactive constituents with potential pharmacological uses, but their use is limited owing to scarce scientific evidence. The in vivo anti-cancer activity of Syringodium isoetifolium against DEN-induced hepatocellular carcinoma in Wistar albino rats is described in this work for the first time. Materials and methods: Wistar albino rats were used as test subjects to examine the anti-cancer properties of Syringodium isoetifolium against DEN-induced hepatocellular carcinoma at the dose of 50 mg/kg body weight. The experimental rats were split into five groups (Group I-V). Except for group I, remaining all animals received DEN and Phenobarbitone during the experiment. Group I and Group II acted as normal and diseased control groups respectively. The extracts were administered to the satellite group III and IV orally with the dose of 250 and 500 mg/kg body weight respectively. 5 fluorouracil 20mg/ kg was administered to group V orally and considered as a standard. The total experimental period lasted for 14 weeks. Results: The findings show that Syringodium isoetifolium significantly reduces liver tumor volume, burden and numbers in experimental rats ( p <0.05) when compared to the control group. Besides, the extracts treated groups restored the pathological parameters close to normal values ( p <0.05). The histological analysis also showed that the extract-treated animals' livers had recovered their normal architecture. Conclusion: The study concludes that Syringodium isoetifolium inhibits the cancer growth in hepatocellular carcinoma by altering the antioxidant defense system, glycolysis and protecting the membrane architecture by inhibiting the elevated levels of haematological, biochemical parameters and biomarker values.
{"title":"Syringodium isoetifolium Fosters an Antioxidant Defense System, Modulates Glycolytic Enzymes and Protects Membrane Integrity in DEN-induced Hepatocellular Carcinoma in Albino Wistar Rats","authors":"D. Kavitha, R. Padmini, M. Dhanaraju, C. Gopi, D. Thiyagarajan, Alekkhya Veeramaneni","doi":"10.5530/ijper.57.3s.78","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.78","url":null,"abstract":"Background: Syringodium isoetifolium seagrass has bioactive constituents with potential pharmacological uses, but their use is limited owing to scarce scientific evidence. The in vivo anti-cancer activity of Syringodium isoetifolium against DEN-induced hepatocellular carcinoma in Wistar albino rats is described in this work for the first time. Materials and methods: Wistar albino rats were used as test subjects to examine the anti-cancer properties of Syringodium isoetifolium against DEN-induced hepatocellular carcinoma at the dose of 50 mg/kg body weight. The experimental rats were split into five groups (Group I-V). Except for group I, remaining all animals received DEN and Phenobarbitone during the experiment. Group I and Group II acted as normal and diseased control groups respectively. The extracts were administered to the satellite group III and IV orally with the dose of 250 and 500 mg/kg body weight respectively. 5 fluorouracil 20mg/ kg was administered to group V orally and considered as a standard. The total experimental period lasted for 14 weeks. Results: The findings show that Syringodium isoetifolium significantly reduces liver tumor volume, burden and numbers in experimental rats ( p <0.05) when compared to the control group. Besides, the extracts treated groups restored the pathological parameters close to normal values ( p <0.05). The histological analysis also showed that the extract-treated animals' livers had recovered their normal architecture. Conclusion: The study concludes that Syringodium isoetifolium inhibits the cancer growth in hepatocellular carcinoma by altering the antioxidant defense system, glycolysis and protecting the membrane architecture by inhibiting the elevated levels of haematological, biochemical parameters and biomarker values.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47477195","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
V. Chaudhari, Shraddha Tawade, S. Nangare, K. Rajput, N. Shirsath, Piyush S. Bafna, L. Zawar
Background: The implementation of chitosan as an enhanced vehicle for drug delivery is an interesting domain in the pharmaceutical dosage form. The combination of commonly accessible natural polysaccharides like gum may provide a new arrangement of dosage forms such as polyelectrolyte complex. Such modern improvements facilitate the modulated release of active, which can be beneficial in avoiding adverse consequences. There have been no reports on chitosan and sesbania gum-based polyelectrolyte complexes for drug delivery applications to date. Objectives: The chitosan-sesbania gum polyelectrolyte complex was developed for modified drug delivery of diclofenac sodium. Materials and Methods: pH-responsive polyelectrolyte complexes were accomplished utilizing the coacervation technique. It forms complex due to the capability of chitosan amine groups and sesbania gum carboxylic functionality. Results: The SEM analysis assured the aggregated polyhedral shape particles with a smooth surface of the final polyelectrolyte complex. The Diffractogram of the polyelectrolyte complex resulted in an amorphous form of diclofenac. The polyelectrolyte complex batch (B:3) showed satisfactory drug entrapment capabilities. It showed 88.96% of the drug release in 8 hr (pH 6.8). Importantly, it is because of the unprotonated condition of sesbania gum containing hydrophilic functionality that offers boosted hydrogen bonding via interaction with dissolution medium containing water molecules. Therefore, it offers the insertion of water molecules into a complex followed by the swelling of a matrix. Conclusion: The developed chitosan-sesbania gum polyelectrolyte complex offers a pH-responsive sustained release of diclofenac sodium. In the future, chitosan and sesbania gum-based polyelectrolyte complex can be preferred as an innovative drug carrier for diclofenac sodium delivery.
{"title":"Chitosan–Sesbania Gum Mediated pH-Responsive Polyelectrolyte Complexes for Targeted Delivery of Diclofenac Sodium: Preparation and Spectroscopical Evaluation","authors":"V. Chaudhari, Shraddha Tawade, S. Nangare, K. Rajput, N. Shirsath, Piyush S. Bafna, L. Zawar","doi":"10.5530/ijper.57.3s.65","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.65","url":null,"abstract":"Background: The implementation of chitosan as an enhanced vehicle for drug delivery is an interesting domain in the pharmaceutical dosage form. The combination of commonly accessible natural polysaccharides like gum may provide a new arrangement of dosage forms such as polyelectrolyte complex. Such modern improvements facilitate the modulated release of active, which can be beneficial in avoiding adverse consequences. There have been no reports on chitosan and sesbania gum-based polyelectrolyte complexes for drug delivery applications to date. Objectives: The chitosan-sesbania gum polyelectrolyte complex was developed for modified drug delivery of diclofenac sodium. Materials and Methods: pH-responsive polyelectrolyte complexes were accomplished utilizing the coacervation technique. It forms complex due to the capability of chitosan amine groups and sesbania gum carboxylic functionality. Results: The SEM analysis assured the aggregated polyhedral shape particles with a smooth surface of the final polyelectrolyte complex. The Diffractogram of the polyelectrolyte complex resulted in an amorphous form of diclofenac. The polyelectrolyte complex batch (B:3) showed satisfactory drug entrapment capabilities. It showed 88.96% of the drug release in 8 hr (pH 6.8). Importantly, it is because of the unprotonated condition of sesbania gum containing hydrophilic functionality that offers boosted hydrogen bonding via interaction with dissolution medium containing water molecules. Therefore, it offers the insertion of water molecules into a complex followed by the swelling of a matrix. Conclusion: The developed chitosan-sesbania gum polyelectrolyte complex offers a pH-responsive sustained release of diclofenac sodium. In the future, chitosan and sesbania gum-based polyelectrolyte complex can be preferred as an innovative drug carrier for diclofenac sodium delivery.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47125425","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Aim: The aim of this research work is the formulation, development and evaluation of Self-Micro Emulsifying Drug Delivery System (SMEDDS). Background: Zileuton, a drug that is poorly soluble in water, was formulated with Tween 20 in a 1:1 ratio as a surfactant. F1 formulation of SMEDDS was selected from the optimum concentration of oils, surfactant, and co-surfactants from psuedoternary diagrams. Materials and Methods: Enaltec Lab in Mumbai, India, provided Zileuton as a gift sample. Raj Chemicals in India provided the eucalyptus oil. Merk Private Ltd., INDIA provided a gift sample of Tween 20. N.R. Traders, INDIA, provided polyethylene glycol 300 (PEG 300). Result: For the optimized formulations, the mean globule size of SMEDDS was found to be below 107 nm, and the zeta potential was negative. The formulations were subjected to various accelerated physical stability tests and self-emulsification evaluations. For investigating drug-excipient interactions, FTIR analysis was carried out. Zileuton in SMEDDS dissolved rapidly and completely in the phosphate buffer pH 7.4 which was used as the dissolution medium, according to the in vitro dissolution data. Conclusion: From the droplet size analysis and zeta potential values confirm the reduction in particle size to nano range which definitely improves the solubility and the dissolution rate.
{"title":"Enhancement of the Solubility of Lipophilic Drug by Self-Micro Emulsifying Drug Delivery System (SMEDDS) For Oral Administration","authors":"P. Gangane, Kiran Singh, Vijaya S. Rabade","doi":"10.5530/ijper.57.3s.59","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.59","url":null,"abstract":"Aim: The aim of this research work is the formulation, development and evaluation of Self-Micro Emulsifying Drug Delivery System (SMEDDS). Background: Zileuton, a drug that is poorly soluble in water, was formulated with Tween 20 in a 1:1 ratio as a surfactant. F1 formulation of SMEDDS was selected from the optimum concentration of oils, surfactant, and co-surfactants from psuedoternary diagrams. Materials and Methods: Enaltec Lab in Mumbai, India, provided Zileuton as a gift sample. Raj Chemicals in India provided the eucalyptus oil. Merk Private Ltd., INDIA provided a gift sample of Tween 20. N.R. Traders, INDIA, provided polyethylene glycol 300 (PEG 300). Result: For the optimized formulations, the mean globule size of SMEDDS was found to be below 107 nm, and the zeta potential was negative. The formulations were subjected to various accelerated physical stability tests and self-emulsification evaluations. For investigating drug-excipient interactions, FTIR analysis was carried out. Zileuton in SMEDDS dissolved rapidly and completely in the phosphate buffer pH 7.4 which was used as the dissolution medium, according to the in vitro dissolution data. Conclusion: From the droplet size analysis and zeta potential values confirm the reduction in particle size to nano range which definitely improves the solubility and the dissolution rate.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41537232","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ammam Abdelkader, B. Reda, Chadli Redouane, Boudia Rafik, Benhafsa Mekhalef Fouad, Hafidh Zemour, D. Villemin, W. Soufan, Fathi Abdellatif Belhouadjeb
Background: Our study consists of a study of the chemical composition of the essential oil administered to a batch of rats undergoing a scorpion sting. Compared with control batches, the nervous state was evaluated by several neurobehavioral tests, namely open classified, dark and light and forced swimming. Materials and Methods: Determination of the composition of the essential oil the plant by GC/MS and its protective effect on the nervous system after exposure of rats to scorpions. Results: of GC/MS show that the chemical composition of this plant is characterized by the dominance of the natural monoterpenoid agent Perilla aldehyde, with a percentage of 70.12%, followed by Limonene (10.10%), Methyleugenol (5.69%), and alpha-Pinene (5.04%). Other compounds such as Perilla alcohol (1.90%), Beta-Pinene (0.61%), Delta-3-Carene (0.59%), Carvone (0.44%) and Camphene (0.33%) were identified only in a small proportion. The series of tests allowed us to see the onset of a depressive state, as well as a significant decrease in locomotor activity in the bitten rats compared to the controls and the treated batch. This hypolocomotor effect is accompanied by a decrease in the animal’s stereotyped behaviours (curiosity, sniffing, biting, and grooming) and muscular tone, which explains the animal’s inability to explore the environment. Conclusion: The neuroprotective power study confirmed the powerful properties of the plant to improve the symptoms caused by the scorpion sting, as proven by several neurobehavioral tests.
{"title":"Chemical Composition and Therapeutic Effects of Ammodicus leucotricus Essential Oils on Neurobehavioral Changes in Wistar Rats after Experimental Scorpion Envenomation","authors":"Ammam Abdelkader, B. Reda, Chadli Redouane, Boudia Rafik, Benhafsa Mekhalef Fouad, Hafidh Zemour, D. Villemin, W. Soufan, Fathi Abdellatif Belhouadjeb","doi":"10.5530/ijper.57.3s.92","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.92","url":null,"abstract":"Background: Our study consists of a study of the chemical composition of the essential oil administered to a batch of rats undergoing a scorpion sting. Compared with control batches, the nervous state was evaluated by several neurobehavioral tests, namely open classified, dark and light and forced swimming. Materials and Methods: Determination of the composition of the essential oil the plant by GC/MS and its protective effect on the nervous system after exposure of rats to scorpions. Results: of GC/MS show that the chemical composition of this plant is characterized by the dominance of the natural monoterpenoid agent Perilla aldehyde, with a percentage of 70.12%, followed by Limonene (10.10%), Methyleugenol (5.69%), and alpha-Pinene (5.04%). Other compounds such as Perilla alcohol (1.90%), Beta-Pinene (0.61%), Delta-3-Carene (0.59%), Carvone (0.44%) and Camphene (0.33%) were identified only in a small proportion. The series of tests allowed us to see the onset of a depressive state, as well as a significant decrease in locomotor activity in the bitten rats compared to the controls and the treated batch. This hypolocomotor effect is accompanied by a decrease in the animal’s stereotyped behaviours (curiosity, sniffing, biting, and grooming) and muscular tone, which explains the animal’s inability to explore the environment. Conclusion: The neuroprotective power study confirmed the powerful properties of the plant to improve the symptoms caused by the scorpion sting, as proven by several neurobehavioral tests.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48850093","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Background: Raltegravir Potassium (RTGP), a BCS class II drug used in the treatment of HIV, has minimal solubility in the aqueous medium, resulting in poor bioavailability; Further, RTGP poor dissolution and limited solubility are also major factors responsible for the significant inter-and intra-patient variability in absorption following oral administration. Objectives: To enhance the solubility of Raltegravir potassium and its free acid using Soluplus ® by solid dispersion technology. Materials and Methods: In the current study, Amorphous Solid Dispersions (ASDs) of RTGP and Raltegravir free acid (RTG) of 20:80% w/w with Soluplus ® (SLP) were prepared using quench cooling. The prepared ASDs analyzed for homogenous single-phase formation and intermolecular interactions employing DSC, XRD, and FT-IR. The drug-polymer miscibility was calculated theoretically as well as experimentally with the aid of Hansen solubility parameter and melting point depression methods. The solubility of the ASDs was evaluated by the shake flask method. Results: Quench cooling yielded an RTGP-SLP and RTG-SLP homogeneous amorphous systems. DSC and XRPD results showed the complete transformation of crystalline to the amorphous phase for ASDs. Intermolecular interactions in specific hydrogen bonding were observed between the carbonyl (-C=O) group of Soluplus ® and the Raltegravir -N-H moiety. RTG solubility in salt solid dispersion increases by 10.7 and 17.4 folds, respectively, compared to pure forms. Furthermore, free acid ASDs improved solubility by 8.7 and 14.1 folds, respectively, compared to their pure compounds. Conclusion: Salt solid dispersion showed a greater extent of miscibility and improved solubility of RTG compared to free acid solid dispersion.
{"title":"Solid State Characterization and Miscibility of Raltegravir in Soluplus Using Solid Dispersion Technology","authors":"Dani Lakshman Yarlagadda, A. M. Nayak, K. Bhat","doi":"10.5530/ijper.57.3s.63","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.63","url":null,"abstract":"Background: Raltegravir Potassium (RTGP), a BCS class II drug used in the treatment of HIV, has minimal solubility in the aqueous medium, resulting in poor bioavailability; Further, RTGP poor dissolution and limited solubility are also major factors responsible for the significant inter-and intra-patient variability in absorption following oral administration. Objectives: To enhance the solubility of Raltegravir potassium and its free acid using Soluplus ® by solid dispersion technology. Materials and Methods: In the current study, Amorphous Solid Dispersions (ASDs) of RTGP and Raltegravir free acid (RTG) of 20:80% w/w with Soluplus ® (SLP) were prepared using quench cooling. The prepared ASDs analyzed for homogenous single-phase formation and intermolecular interactions employing DSC, XRD, and FT-IR. The drug-polymer miscibility was calculated theoretically as well as experimentally with the aid of Hansen solubility parameter and melting point depression methods. The solubility of the ASDs was evaluated by the shake flask method. Results: Quench cooling yielded an RTGP-SLP and RTG-SLP homogeneous amorphous systems. DSC and XRPD results showed the complete transformation of crystalline to the amorphous phase for ASDs. Intermolecular interactions in specific hydrogen bonding were observed between the carbonyl (-C=O) group of Soluplus ® and the Raltegravir -N-H moiety. RTG solubility in salt solid dispersion increases by 10.7 and 17.4 folds, respectively, compared to pure forms. Furthermore, free acid ASDs improved solubility by 8.7 and 14.1 folds, respectively, compared to their pure compounds. Conclusion: Salt solid dispersion showed a greater extent of miscibility and improved solubility of RTG compared to free acid solid dispersion.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42446578","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Amit Godbole, Rita Wadetwar, S. Bundale, N. Nashikkar, Pranita S. Kanojiya
Background: Actinomycetes are unique and ubiquitous organisms in nature and are historically holding first position as one of the major antibiotic producers. The aim of the study was screening and pre-treatments of soil, marine, and mangrove samples for isolation of antibiotic producing actinomycetes. Materials and Methods: Actinomycetes were isolated from pre-treated soil, marine, and mangrove samples using different isolation media. They were assessed for antimicrobial activity by cross streak and agar well diffusion method. Colony characteristics, growth pattern and microscopy were performed for partial characterization of the isolates. Promising isolates were identified by 16S rRNA genomic analysis and deposited in GenBank. Results: Study led to the isolation of 109 actinomycete isolates. In the microbiological studies, 19 isolates showed a potent inhibition against E. coli , 17 isolates showed activity against S. aureus , 10 isolates exhibited activity against K. pneumoniae and B. subtilis each, and 9 isolates showed activity against C . albicans . The results revealed that most of the isolates belonged to Streptomyces genus. Less than 10% isolates belonged to non-Streptomyces genera. The broad-spectrum antimicrobial activity against all the test organisms was exhibited by 6 soil isolates designated as D, D2, F30 (brown pigment), TS13 (pink), TS14 (green), TS4 (cherry red), and 5 marine isolate M1, M7 (pink), M10, M14, M11 (yellow). Conclusion: Our findings highlights that the West coast and mangrove forest of Maharashtra are attractive sites to knock out the biologically active and undiscovered species of actinomycetes having potential to produce novel antibiotic.
{"title":"Bioprospecting of Actinomycetes from Diverse Ecosystems for Antimicrobial Activity","authors":"Amit Godbole, Rita Wadetwar, S. Bundale, N. Nashikkar, Pranita S. Kanojiya","doi":"10.5530/ijper.57.3s.68","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.68","url":null,"abstract":"Background: Actinomycetes are unique and ubiquitous organisms in nature and are historically holding first position as one of the major antibiotic producers. The aim of the study was screening and pre-treatments of soil, marine, and mangrove samples for isolation of antibiotic producing actinomycetes. Materials and Methods: Actinomycetes were isolated from pre-treated soil, marine, and mangrove samples using different isolation media. They were assessed for antimicrobial activity by cross streak and agar well diffusion method. Colony characteristics, growth pattern and microscopy were performed for partial characterization of the isolates. Promising isolates were identified by 16S rRNA genomic analysis and deposited in GenBank. Results: Study led to the isolation of 109 actinomycete isolates. In the microbiological studies, 19 isolates showed a potent inhibition against E. coli , 17 isolates showed activity against S. aureus , 10 isolates exhibited activity against K. pneumoniae and B. subtilis each, and 9 isolates showed activity against C . albicans . The results revealed that most of the isolates belonged to Streptomyces genus. Less than 10% isolates belonged to non-Streptomyces genera. The broad-spectrum antimicrobial activity against all the test organisms was exhibited by 6 soil isolates designated as D, D2, F30 (brown pigment), TS13 (pink), TS14 (green), TS4 (cherry red), and 5 marine isolate M1, M7 (pink), M10, M14, M11 (yellow). Conclusion: Our findings highlights that the West coast and mangrove forest of Maharashtra are attractive sites to knock out the biologically active and undiscovered species of actinomycetes having potential to produce novel antibiotic.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46221768","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
N. Shah, R. Prajapati, D. Gohil, C. Aundhia, Piyushkumar Sadhu, S. Kardani
Aim/Background: This research work intended to make use of prospective advantages of niosomes for the improvement in topical delivery of poorly soluble luliconazole. Materials and Methods: Luliconazole, an anti-fungal agent used in the treatment of fungal infection, was successfully formulated as niosomal topical gel by using a polymer carbopol 934. The 3 2 full factorial statistical design was employed as a means for the optimization of niosomal formulation to check the impact of two formulation factors namely, concentration of cholesterol and span 60 on two dependent variables % drug release and % drug entrapment efficiency in formulated niosomal formulations. Results: The mean vesicular size, Zeta potential, drug release and entrapment efficiency of optimized formulation was found 150.6 ± 11.1 nm, -23.5 ± 5.08, 92.41 ± 2.44% and 92.36 ± 2.85%, respectively. The scanning electron microscopy study reveals that the optimized formulation was spherical, porous and rough in surface. The thermogram of differential scanning calorimetry study states that the drug may be solubilise or converted to amorphous form in niosomal vesicles. The viscosity and spreadability of niosomal gel were observed satisfactorily for the easy topical application. The ex vivo study of optimized niosomal gel showed significant higher drug release (97.31 ± 3.18%) in comparison with marketed product (82.20 ± 1.95%). The antifungal study showed considerable antifungal effectiveness of niosomal gel against the conventional marketed preparation. Conclusion: Henceforth, it can be concluded that the niosomes loaded topical gel of luliconazole may be useful for reducing the application frequency of conventional topical product and thereby improves the patient compliance.
{"title":"Luliconazole Loaded Niosomal Topical Gel: Factorial Design, in vitro Characterization and Antifungal Study","authors":"N. Shah, R. Prajapati, D. Gohil, C. Aundhia, Piyushkumar Sadhu, S. Kardani","doi":"10.5530/ijper.57.3s.60","DOIUrl":"https://doi.org/10.5530/ijper.57.3s.60","url":null,"abstract":"Aim/Background: This research work intended to make use of prospective advantages of niosomes for the improvement in topical delivery of poorly soluble luliconazole. Materials and Methods: Luliconazole, an anti-fungal agent used in the treatment of fungal infection, was successfully formulated as niosomal topical gel by using a polymer carbopol 934. The 3 2 full factorial statistical design was employed as a means for the optimization of niosomal formulation to check the impact of two formulation factors namely, concentration of cholesterol and span 60 on two dependent variables % drug release and % drug entrapment efficiency in formulated niosomal formulations. Results: The mean vesicular size, Zeta potential, drug release and entrapment efficiency of optimized formulation was found 150.6 ± 11.1 nm, -23.5 ± 5.08, 92.41 ± 2.44% and 92.36 ± 2.85%, respectively. The scanning electron microscopy study reveals that the optimized formulation was spherical, porous and rough in surface. The thermogram of differential scanning calorimetry study states that the drug may be solubilise or converted to amorphous form in niosomal vesicles. The viscosity and spreadability of niosomal gel were observed satisfactorily for the easy topical application. The ex vivo study of optimized niosomal gel showed significant higher drug release (97.31 ± 3.18%) in comparison with marketed product (82.20 ± 1.95%). The antifungal study showed considerable antifungal effectiveness of niosomal gel against the conventional marketed preparation. Conclusion: Henceforth, it can be concluded that the niosomes loaded topical gel of luliconazole may be useful for reducing the application frequency of conventional topical product and thereby improves the patient compliance.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48905665","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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