International Journal of Applied Pharmaceutics最新文献_第4页

UTILIZATION RED DRAGON FRUIT PEEL (HYLOCEREUS POLYRHIZUS) ETHANOL EXTRACT IN ORAL THIN FILM STRIP AS A MOUTH FRESHENER 利用红龙果皮（hylocereus polyrhizus）乙醇提取物口服薄膜条作为口腔清新剂

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50043

Nabila Apriliani, L. Laila, B. Prasetyo

{"title":"UTILIZATION RED DRAGON FRUIT PEEL (HYLOCEREUS POLYRHIZUS) ETHANOL EXTRACT IN ORAL THIN FILM STRIP AS A MOUTH FRESHENER","authors":"Nabila Apriliani, L. Laila, B. Prasetyo","doi":"10.22159/ijap.2024v16i3.50043","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50043","url":null,"abstract":"Objective: The aim of this study was to formulate an oral thin film strip (OTFS) contained the red dragon fruit peel (RDFP) ethanol extract (Hylocereus polyrhizus) and evaluate the characteristic, stability and antibacterial activity against Streptococcus mutans (S. mutans).\u0000Methods: The film was made using the solvent casting method by adding a variety of concentration ethanol extract of red dragon fruit peel (5%, 10%, and 15%). The films were evaluated in organoleptic test, weight, thickness, pH, disintegration time, folding endurance, stability test and antibacterial activity.\u0000Results: The results showed that the film provided a distinctive color, aroma, and taste of the extract. The result of film evaluation had weight between 0.07-0.21 g, thickness between 0.10-0.20 mm, pH between 5.70-5.99, disintegration time between 34.99-49.13 s, and folding endurance between 321.00-812.83 times. The films were stable for 2 mo at a variety storage temperature (4±2 ℃, 28±2 ℃, and 40±2 ℃). The films showed antibacterial activity for 5%, 10% and 15% with the diameter of inhibition 8.5 mm, 10.8 mm, and 12.9 mm, respectively.\u0000Conclusion: Ethanol extract of RDFP can be utilized as a mouth freshener film that is stable for 2 mo and has antibacterial activity against S. mutans.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"10 27","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004778","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}

引用次数: 0

IBUPROFEN INJECTABLE MICROEMULSION PREPARATION COATED BY CHITOSAN: FORMULATION, CHARACTERIZATION, IN VITRO PERFORMANCE, ANTI-INFLAMMATION ACTIVITY, AND HEMATOLOGY ASSESSMENT 壳聚糖包衣的布洛芬注射用微乳剂制剂：配方、表征、体外性能、抗炎活性和血液学评估

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50220

Aulia UL HAFIZAH, Purwantiningsih Sugita, Mohammad Khotib, Umi Cahyaningsih, Siti Sadiah

{"title":"IBUPROFEN INJECTABLE MICROEMULSION PREPARATION COATED BY CHITOSAN: FORMULATION, CHARACTERIZATION, IN VITRO PERFORMANCE, ANTI-INFLAMMATION ACTIVITY, AND HEMATOLOGY ASSESSMENT","authors":"Aulia UL HAFIZAH, Purwantiningsih Sugita, Mohammad Khotib, Umi Cahyaningsih, Siti Sadiah","doi":"10.22159/ijap.2024v16i3.50220","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50220","url":null,"abstract":"Objective: This study aimed to develop, characterize, and conduct stability evaluations to ensure compliance with intravenous administration for microemulsion ibuprofen injection. In addition, hematology assessment and profile of drug release kinetics were analyzed.\u0000Methods: The formulation process commenced by introducing various chitosan concentrations into microemulsion ibuprofen injection, following a method established in a previous study. Formulation parameters studied include particle size, polydispersity index (PDI), zeta potential, kinetic of drug release, anti-inflammation activity using the 1% carrageenin induction method, and hematology assessment.\u0000Results: The results showed that the addition of 1% chitosan solution allowed for the development of the ideal microemulsion formula, with droplet size, zeta potential, and PDI of 19.37±0.32 nm,-1.53±0.12 mV, and 0.38±0.02, respectively. Kinetics of chitosan-coated ibuprofen microemulsion (MK) were governed by the squared root of time paradigm, suggesting that drug release proceeded by diffusion and was influenced by the carrier. Compared to the other groups, the paw injected with MK indicated a strong anti-inflammatory effect and did not differ significantly from the control group (p>0.05). However, Hematology analysis showed no statistically significant variations in leukocyte and erythrocyte profiles between the treatment and control groups (p>0.05).\u0000Conclusion: MK met the criteria as an intravenous preparation based on the characteristics and safety.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"23 38","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004791","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}

引用次数: 0

FORMULATION OF NANOPARTICLE CONTAINING KENIKIR LEAF ETHANOL EXTRACTS (COSMOS CAUDATUS KUNTH.) AND ANTIDIABETIC ACTIVITY IN RATS 含有凯尼基尔叶乙醇提取物（Cosmos caudatus kunth.）的纳米粒子配方和大鼠的抗糖尿病活性

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.49980

D. Wijaya, Raden Ayu Aulya Herlina, Azizan Haq

{"title":"FORMULATION OF NANOPARTICLE CONTAINING KENIKIR LEAF ETHANOL EXTRACTS (COSMOS CAUDATUS KUNTH.) AND ANTIDIABETIC ACTIVITY IN RATS","authors":"D. Wijaya, Raden Ayu Aulya Herlina, Azizan Haq","doi":"10.22159/ijap.2024v16i3.49980","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.49980","url":null,"abstract":"Objective: This study aimed to formulate the ethanol extract of kenikir leaf into nanoparticles. The ethanol extract of kenikir leaves loading into nanoparticles can enhanced the stability and effectiveness of antidiabetic activity.\u0000Methods: The nanoparticles were prepared using the ionic gelation method with chitosan and variation in sodium tripolyphosphate. The nanoparticle formula was characterized by efficiency encapsulation using spectrophotometry methods and particle size, zeta potential, and polydispersity index using dynamic light scattering (DLS). An antidiabetic activity test was initiated by inducing a high-fat and fructose diet. The parameters tested were decreasing blood glucose levels in rats.\u0000Results: The result of the characterization of the nanoparticle was the percent of efficiency encapsulation, particle size, PDI, zeta potential, and pH were carried out to get the best formula. The best formula obtained was the percent of efficiency encapsulation of 96.20±0.0278%, the particle size of 144.6±7.800 nm, zeta potential of+15.32±0.9550 mEv, PDI of 0.48±0.070, and pH of 4.255±0.0035. The decrease in blood glucose levels in the nanoparticles of kenikir leaves extract was not significantly (p>0.05) different from the positive group (metformin) compared to the kenikir leaves extract, which decreased not really significantly.\u0000Conclusion: Nanoparticle containing kenikir leaf ethanol extract successfully prepared into nanoparticles and the potential to increase antidiabetic activity.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"68 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003382","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}

引用次数: 0

QUANTITATIVE DETERMINATION OF SOME NON-STEROIDAL ANTI-INFLAMMATORY DRUGSAND THEIR ACID DISSOCIATION CONSTANTS BY DIRECT POTENTIOMETRY 通过直接电位测定法定量测定一些非甾体类消炎药及其酸解离常数

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50111

V. Maslarska

{"title":"QUANTITATIVE DETERMINATION OF SOME NON-STEROIDAL ANTI-INFLAMMATORY DRUGSAND THEIR ACID DISSOCIATION CONSTANTS BY DIRECT POTENTIOMETRY","authors":"V. Maslarska","doi":"10.22159/ijap.2024v16i3.50111","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50111","url":null,"abstract":"Objective: A potentiometric titration method was applied to determine non-steroidal anti-inflammatory drugs. The quantitative analysis and the treatment of the primary data are based on a nonlinear regression procedure using commercial software. A general formula valid for every type of acid-base titration, derived before is used as a direct input.\u0000Methods: Potentiometric titration of ibuprofen, flurbiprofen, and ketoprofen with sodium hydroxide solution (0.1 mol/l). The solutions of ibuprofen, flurbiprofen, and ketoprofen were prepared in solvent CH3OH: H2O (40:60%). The determination was carried out using a 713 Metrohm pH meter, equipped with Metrohm combined electrode ref. 6.0228.000 Pt1000 with temperature sensor and auto burette. The analysis was performed at ionic strength (I=0.2 mol/l KCl) and t = 25±0.2 °C.\u0000Results: The discussed substances were analyzed using potentiometric titration with a standard sodium hydroxide solution (0.1 mol/l). The experimental data V, ml/E, mV and the conditions of these titrations were used as input in the Data Fit program fixing the following parameters Vo =100.0 ml; Ct (NaOH) = 0.1000 mol/l; S = 59.16 mV (corresponding to 25 °C theoretical value) and Kw = 1.2 10-14 (ionic strength 0.2 mol/l). The analytical results for ibuprofen, flurbiprofen and ketoprofen were determined with good accuracy (error+0.4 % foribuprofen+0.2 % for flurbiprofen and+0.2 % for ketoprofen) and precision (1 % for the three). The quantity and acid-base constants of ibuprofen, flurbiprofen, and ketoprofen were determined alone and in tablets. The validation of the method showed very good accuracy and precision.\u0000Conclusion: The present approach can be successfully used in routine analysis of the study drugs in quality control laboratories.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"11 18","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004509","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}

引用次数: 0

FORMULATION AND STABILITY EVALUATION OF ANTI-OBESITY NUTRACEUITCAL BLEND OF WHITE KIDNEY BEAN EXTRACT (PHASEOLUS VULGARIS L.), PROPOLIS ETHANOLIC EXTRACT AND CRPIC3 白芸豆提取物（Phaseolus vulgaris L.）、蜂胶乙醇提取物和 Crpic3 的抗肥胖营养混合物的配方和稳定性评价

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50705

Doaa Salah ELDIN ABDELFATTAH, Mervat A Fouad, Aliaa N Elmeshad, M. EL-NABARAWI, S. F. Elhabal

{"title":"FORMULATION AND STABILITY EVALUATION OF ANTI-OBESITY NUTRACEUITCAL BLEND OF WHITE KIDNEY BEAN EXTRACT (PHASEOLUS VULGARIS L.), PROPOLIS ETHANOLIC EXTRACT AND CRPIC3","authors":"Doaa Salah ELDIN ABDELFATTAH, Mervat A Fouad, Aliaa N Elmeshad, M. EL-NABARAWI, S. F. Elhabal","doi":"10.22159/ijap.2024v16i3.50705","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50705","url":null,"abstract":"Objective: This study aimed to formulate and evaluate the stability profile of an anti-obesity nutraceutical combination in different dosage forms.\u0000Methods: Active and inactive ingredients were formulated into pharmaceutical dosage forms. The quality parameters of the dosage forms were determined, followed by accelerated stability testing (40±2 °C and 75±5% Relative Humidity (RH)) for 180 d was completed to evaluate their physical, chemical and microbiological attributes throughout the storage period.\u0000Results: Pre-formulation parameters of the powder blend of active and inactive ingredients for each dosage form showed a satisfactory flowability with Hausner's ratio falling between 1.16 and 1.18, average angle of repose between 22.29° and 22.90° and acceptable compressibility with Carr’s index below 25%. Tablets assessments were acceptable with a mean friability value of 0.21±0.03%, hardness of 4.12±0.09 kg/cm2. The average disintegration time of 5 min 10 sec for tablets and 4 min and 30 sec for capsules. The accelerated stability study revealed that tablet dosage forms are stable for longer period that can reach up to 180 d (24 mo real-time), while sachets and capsules are stable for a period of 135 d (18 mo real-time).\u0000Conclusion: The anti-obesity blend of White Kidney Bean Extract (WKBE), Propolis Ethanolic Extract (PEE) and CrPic3 can be successfully formulated in acceptable and convenient dosage forms that can be stable for 18-24 mo.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"87 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003333","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}

引用次数: 0

DEVELOPMENT AND OPTIMIZATION OF RABEPRAZOLE CHRONO-MODULATED DRUG DELIVERY SYSTEMS 开发和优化雷贝拉唑慢性调节给药系统

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50189

Phaneendra Kurapati, Santhivardhan Chinni

{"title":"DEVELOPMENT AND OPTIMIZATION OF RABEPRAZOLE CHRONO-MODULATED DRUG DELIVERY SYSTEMS","authors":"Phaneendra Kurapati, Santhivardhan Chinni","doi":"10.22159/ijap.2024v16i3.50189","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50189","url":null,"abstract":"Objective: Development and optimization of chrono-modulated pulsatile drug delivery systems (CPDDS) loaded with Rabeprazole for treating nocturnal acid breakthrough in ulcer patients was set as the major objective of this work.\u0000Methods: CPDDS were developed to provide drug release as two pulses with predetermined gap. Separate microparticles for delayed instant release (DIR) and delayed extended-release (DER) were formulated. Through the optimization of several formulation and process parameters, ER microparticles were created as matrix microspheres. Central composite design was used to understand how the factors affected the responses. The optimized ER microspheres and plain drug were separately subjected to enteric coating to obtain DER and DIR portion microparticles, respectively.\u0000Results: With the exception of stirring speed's impact on drug release, every other factor was found to have a significant influence (p<0.05) on every response. The mechanism underlying the Rabeprazole's delayed prolonged release was explained by the SEM images. The microspheres made with Eudragit RSPO at 0.72 g and polyethylene oxide at 0.5 g for 1 g of Rabeprazole at 400 rpm were shown to be the optimal formulation based on the graphical optimization results. After being coated with a terminal enteric coating, this formulation showed delayed release for a duration of 6 h.\u0000Conclusion: After oral administration of equal doses of DIR microcapsules along with the optimized DER microspheres could release Rabeprazole effectively as two different pulses at the desired time intervals.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004886","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}

引用次数: 0

PREDICTION OF SULFAMETHOXAZOLE AND TRIMETHOPRIM PLASMA LEVELS FROM TABLETS AND DISSOLUTION MEDIA OF PHYSIOLOGICAL RELEVANCE 通过药片和具有生理意义的溶解介质预测磺胺甲噁唑和三甲氧苄嘧啶的血浆水平

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50409

Jose Manuel RIOS-RODRIGUEZ, Felipe Dino REYES-RAMIREZ, J. C. RUIZ-SEGURA, J. R. MEDINA-LÓPEZ

{"title":"PREDICTION OF SULFAMETHOXAZOLE AND TRIMETHOPRIM PLASMA LEVELS FROM TABLETS AND DISSOLUTION MEDIA OF PHYSIOLOGICAL RELEVANCE","authors":"Jose Manuel RIOS-RODRIGUEZ, Felipe Dino REYES-RAMIREZ, J. C. RUIZ-SEGURA, J. R. MEDINA-LÓPEZ","doi":"10.22159/ijap.2024v16i3.50409","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50409","url":null,"abstract":"Objective: To estimate plasma concentrations-time profiles of Sulfamethoxazole (SMZ) and Trimethoprim (TMP) from fixed-dose combination formulations through in vitro data of dissolution media of physiological relevance and a convolution model.\u0000Methods: Dissolution profiles of SMZ/TMP tablets (400/80 mg) were obtained with USP paddle apparatus at 100 rpm and 900 ml of 0.1 N HCl, pH 4.5 acetate buffer, and pH 6.8 phosphate buffer. The reference drug product and two generic formulations were tested. Drugs were quantified by a derivative method. Dissolution profiles were compared with model-dependent and independent methods. SMZ/TMP plasma levels were simulated with dissolution data and published in vivo information. Percent of prediction error (PE) for peak plasma concentration (Cmax) and area under the curve from zero time to infinity (AUC0-inf) at each condition were calculated.\u0000Results: In all used conditions, similar dissolution profiles were found excepting for TMP at pH 1.2 (f2<50). The in vitro release performance for reference and generic formulations was explained by the Weibull function only for SMZ at pH 6.8 and TMP at pH 4.5. Values of PE>19% for both generic formulations were found with TMP at pH 1.2.\u0000Conclusion: Significant differences in TMP dissolution profiles of generic formulations at pH 1.2 reflect the subsequent differences found in predicted Cmax and AUC0-inf.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"62 s286","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003226","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}

引用次数: 0

SINUSOIDAL ELECTROMAGNETIC FIELD DECREASES OSTEOGENIC DIFFERENTIATION OF RAT BONE MARROW MESENCHYMAL STEM CELLS 正弦电磁场会降低大鼠骨髓间充质干细胞的成骨分化能力

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50382

Dhiya Altememy, Maryam Haji GHASEM KASHANI, Osamah N. WENAS

{"title":"SINUSOIDAL ELECTROMAGNETIC FIELD DECREASES OSTEOGENIC DIFFERENTIATION OF RAT BONE MARROW MESENCHYMAL STEM CELLS","authors":"Dhiya Altememy, Maryam Haji GHASEM KASHANI, Osamah N. WENAS","doi":"10.22159/ijap.2024v16i3.50382","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50382","url":null,"abstract":"Objective: The widespread use of household electrical appliances generating electric and magnetic fields was a significant focus of WHO attention because of its serious threat to human health, especially osteogenesis. This research investigated the effect of 50 Hz frequency (1 mT intensity) sinusoidal EMF (SEMF) on the osteogenic differentiation of rat bone marrow stem cells (rBMSCs) in vitro.\u0000Methods: Experimental groups were: positive control (cells cultured in osteogenic medium supplemented with 7-10 M Dexamethasone, negative control (cells cultured in α-MEM/10% FBS, 10 mmol Beta-Glycerol-Phosphate, 15% FBS, 50 ug/ml Ascorbic Acid bi-Phosphate, 100 unit/ml Penicillin) and for the EMF group, cells exposed to SEMF (50 Hz, 1 mT, 30 min/day) for 14 and 21 d. Alizarin red staining, Alkaline phosphatase activity, and QRT-PCR were performed.\u0000Results: The EMF group exhibited weaker positive stains for ALP and Alizarin red than the positive control group. The Runx2 and Ocn gene expression levels were significantly decreased compared to negative control at 14 and 21 d of EMF exposure, respectively. After 14 and 21 d of exposure, Runx2 and Ocn gene expression were much lower in the EMF group than in the positive control group.\u0000Conclusion: SEMF (1 mT, 50 Hz, 30 min/day) could retarded osteogenesis and reduce the osteogenic differentiation of rBMSCs.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"70 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003366","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}

引用次数: 0

ENHANCING NOSE- TO- BRAIN DELIVERY OF PIRIBEDIL: DEVELOPMENT OF A NANOSUSPENSION DISPERSED IN NASAL IN-SITU GELLING SYSTEM 加强吡贝地尔的鼻脑给药：开发一种分散在鼻腔原位胶凝系统中的纳米悬浮剂

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50242

Chekkilla Bhargavi, P. Raghuveer

{"title":"ENHANCING NOSE- TO- BRAIN DELIVERY OF PIRIBEDIL: DEVELOPMENT OF A NANOSUSPENSION DISPERSED IN NASAL IN-SITU GELLING SYSTEM","authors":"Chekkilla Bhargavi, P. Raghuveer","doi":"10.22159/ijap.2024v16i3.50242","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50242","url":null,"abstract":"Objective: This study focuses on improving the delivery of Piribedil, a poorly soluble drug, to the brain through the nasal route using a nanosuspension in a nasal in-situ gel.\u0000Methods: The nanosuspension was prepared using the sonoprecipitation method. Quality-by-Design (QbD) principles were used to optimize both the formulation and process parameters. The optimal process parameters were determined as sonication time (7.09 min), sonication amplitude (83.44%), and infusion rate (2.41 mL/min) with a desirability value of 0.970.\u0000Results: The nanosuspension exhibited an average particle size ranging from 46.7 nm to 50.1 nm, and polydispersity index values between 0.393 and 0.425. Zeta potential values ranged from -33.78 ± 1.86 mV to -35.06 ± 2.12 mV, indicating favorable stability. FTIR studies revealed molecular interactions between Piribedil and stabilizers. XRPD and DSC analyses showed the transition from a crystalline to an amorphous state in the nanosuspension. Dissolution studies demonstrated significantly accelerated dissolution for the Piribedil nanosuspension, attributed to its nanosize and improved wettability. Stability assessments confirmed the robustness of the nanosuspension.\u0000Conclusion: This innovative approach offers potential solutions for drug solubility challenges and blood-brain barrier penetration, holding promise for effective brain-targeted treatments.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"69 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003375","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}

引用次数: 0

STUDY OF THE INHIBITORY EFFECTS OF VITAMIN E DERIVATIVES ON MITOCHONDRIAL COMPLEX II SUBUNIT USING MOLECULAR DOCKING 利用分子对接研究维生素 e 衍生物对线粒体复合体 II 亚基的抑制作用

International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50040

Irma Ratna Kartika, Teni Ernawati, S. A. Jusman, M. Sadikin

{"title":"STUDY OF THE INHIBITORY EFFECTS OF VITAMIN E DERIVATIVES ON MITOCHONDRIAL COMPLEX II SUBUNIT USING MOLECULAR DOCKING","authors":"Irma Ratna Kartika, Teni Ernawati, S. A. Jusman, M. Sadikin","doi":"10.22159/ijap.2024v16i3.50040","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50040","url":null,"abstract":"Objective: The goal of this study was to create vitamin E derivatives and explore their potential anticancer properties using a computational approach.\u0000Methods: The Steglich method was used for the synthesis of the vitamin E-fatty acid (pentanoic acid, heptanoic acid, and octanoic acid) derivatives, with N,N'-dicyclohexylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP) as the catalysts. The structure of the synthesized products was determined by ultraviolet-visible (UV-Vis) spectroscopy, fourier transform infrared (FTIR) spectroscopy, and liquid chromatography-mass spectrometry (LC-MS). Molecular docking was carried out on the succinate dehydrogenase (SDH) enzyme using AutoDockTools.\u0000Results: α–Tocopherol pentanoate (α–TP), α–tocopherol heptanoate (α–TH), and α–tocopherol octanoate (α–TO) were the three vitamin E derivatives synthesized in this study. Based on the results of molecular docking, the novel compounds (α–TP, α–TH, and α–TO) generated bond energies of-10.57,-9.61, and-9.20 kcal/mol, respectively.\u0000Conclusion: All newly synthesized compounds exhibited lower binding affinity values than α–tocopherol (α–T). This confirms that these compounds might not provide greater advantages than α-tocopherol in terms of inhibitory effects on mitochondrial complex II (CII).","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"50 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003246","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}

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