scholarly journals Formulation and Characterization of Nimodipine Nanoparticles for the Enhancement of solubility and dissolution rate

2021 ◽  
Vol 30 (2) ◽  
pp. 143-152
Author(s):  
Areej Wahhab Alhagiesa ◽  
Mowafaq M. Ghareeb
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Channel Blocker ◽  
Polymeric Nanoparticles ◽  
Poloxamer 407 ◽  
High Permeability ◽  
Freeze Dried ◽  
Dihydropyridine Calcium Channel Blocker ◽  
Low Solubility

Nimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which  Soluplus  has been utilized as a stabilizer, has a particle size (77 nm) and polydispersity index (PDI) (0.016). The formulas with the smallest particle size were freeze dried with the addition of 1 % w/w mannitol as cryoprotectant. The saturation solubility of NMD in the prepared nanoparticles was increased twenty four-folds, and the complete dissolution was achieved at 90 minutes compared with pure NMD, which reaches only 6%. The formation of hydrogen bonding between NMD and the polymer or the cryoprotectant, as confirmed by the FTIR study. In conclusion, the preparation of NMD as polymeric nanoparticles is a useful technique for enhancing the solubility and dissolution rate.

scholarly journals Solubility Enhancement of Clozapine Through Co-Crystal Formation with Isonicotinamide

2019 ◽  
Vol 2 (1) ◽  
Author(s):  
Fikri Alatas ◽  
Hestiary Ratih ◽  
Hesti Kurnia ◽  
Sundani Nurono Soewandhi
Keyword(s):  
Dissolution Rate ◽  
Phosphate Buffer Solution ◽  
Crystal Formation ◽  
X Ray Diffraction ◽  
High Permeability ◽  
Buffer Solution ◽  
Pxrd Pattern ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

Clozapine (CLO) is an effective atypical antipsychotic to control the symptoms of psychosis and schizophrenia. Clozapine has low solubility and high permeability, so it is classified as a class II in the biopharmaceutical classification system. The aim of this study was to improve the solubility and dissolution rate of clozapine by clozapine-isonicotinamide (CLO-INA) co-crystal formation. CLO-INA co-crystal was prepared by solvent-drop grinding (SDG) method using water as a solvent. Characterization of SDG result was conducted by powder X-ray diffraction (PXRD) and Fourier transform infrared (FTIR).  Solubility test was performed in water at room temperature. The dissolution test was performed in 900 mL of pH 6.8 phosphate buffer solution, 50 rotation per minute of paddle rotation, and at 37±0.5 °C. The PXRD pattern of  SDG result of CLO-INA has many different peaks from its parent components, and this may indicate the co-crystal formation. The solubility of the co-crystal clozapine was fifteen folds higher than pure clozapine. The dissolution rate of CLO-INA co-crystal increased in the first 10 minutes compared to pure clozapine. Percentage of clozapine dissolved after 10 minutes from CLO-INA co-crystal and pure CLO were 10.2 and 2.4%, respectively. CLO and INA can form co-crystal by SDG method that can improve the solubility and dissolution rate of clozapine.Keywords: Clozapine, Isonicotinamide, Co-crystal, Solubility, Dissolution

scholarly journals Review: Solid Dispersion of Fenofibrate Using Poly Ethylene Glycol 6000

2021 ◽  
Vol 6 (6) ◽  
pp. 42-51
Author(s):  
Nelvia Helsinta ◽  
Auzal Halim ◽  
Maria Dona Octavia ◽  
Harrizul Rivai
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Literature Search ◽  
Solid Dispersions ◽  
Poly Ethylene Glycol ◽  
Peg 6000 ◽  
Poly Ethylene ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

This review aimed to find information about the solubility of the fenofibrate solid dispersion system using PEG 6000. Fenofibrate is an antihyperlipidemic drug that belongs to the Biopharmaceutical Classification System Class II (BCS II) with low solubility. To find information was by conducting a literature search in national and international journals in the last ten years (2010-2020) through websites, namely Google Scholar, Science Direct, NCBI, ResearchGate, and other trusted journals. Several keywords were used as follows: fenofibrate, solid dispersion, PEG 6000, and dissolution rate. The results of several research journals showed that the solid dispersion of fenofibrate using PEG 6000 made by various methods causes a reduction in particle size to increase the solubility and dissolution rate of fenofibrate. The solid dispersions system was made using several methods, namely fusion (melting), solvent evaporation, dropping, and co-grinding, which is a technique used to increase the solubility of a drug. PEG 6000 was chosen as the carrier because it has high hydrophilicity, is non-toxic, inert, economical, has a low melting point, and is dense at melting temperature to withstand crystallization. Thus it can be concluded that the manufacture of solid dispersion of fenofibrate using PEG 6000 and several methods showed the same results, namely an increase in solubility and dissolution rate.

Design, Fabrication and Characterization of Esomeprazole Nanocrystals for Enhancing the Dissolution Rate and Stability

2020 ◽  
Vol 14 ◽  
Author(s):  
Vijay Agarwal ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Crystalline State ◽  
Physical Mixture ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Physical Treatment ◽  
Pxrd Pattern ◽  
Freeze Dried ◽  
Bulk Drug

Background: Poor solubility and low dissolution rate limit the work at poorly water-soluble drugs like Esomeprazole. To overcome this problem, different technologies had to be used but could not resolve the problem, significantly. The main aim of this study was to prepare the nanocrystals using evaporative precipitation ultrasonication method in order to improve the dissolution rate and stability of Esomeprazole (ESM). Methods: For getting the nanocrystals, different nanoformulations were prepared using the pluronic F-68 in different concentration, and then screened formulation was lyophilized in presence of two distinct cryoprotectants; mannitol and sucrose. The obtained nanocrystals were characterized for their re-dispersibility, crystalline state, dissolution behavior, particle size, polydispersibility index and morphology. Dissolution study of ESM nanocrystals was performed in buffer solution of pH-7.4, and compare to that of bulk ESM sample and ESM/pluronic F-68 physical mixture. Results: Cryoprotectant containing nanocrystals exhibit the re-dispersion in water after the manual shaking. 5% mannitol containing nanocrystals showed the least polydispersity index (0.42 ± 0.11) and narrowest particle size (186 ± 12.9 nm). The powder x-ray diffraction (PXRD) pattern and differential scanning calorimeter (DSC) thermograms revealed that crystalline state of drug was not changed after the different physical treatment. Freeze-dried nanocrystals showed a faster dissolution rate and almost 99.45% of drug was released within 60 min. However, the bulk drug and a physical mixture of bulk drug/pluronic F-68 showed only 22.65% and 21.3% of drug release, respectively, after 60 min. Conclusion: The different findings revealed that nanocrystals could be a potential alternate for solving the dissolution rate and stability issue of ESM like poorly soluble drugs.

Enhancement of the solubility of asenapine maleate through the preparation of co-crystals

2021 ◽  
Vol 18 ◽  
Author(s):  
Suhair S. Al-Nimry ◽  
Mai S. Khanfar
Keyword(s):  
Dissolution Rate ◽  
Exothermic Peak ◽  
In Vitro Dissolution ◽  
High Permeability ◽  
Drug Bioavailability ◽  
Evaporation Technique ◽  
Lower Melting Point ◽  
Rate Limiting ◽  
Low Solubility

Background: Asenapine maleate, an anti-schizophrenic drug, is a class II drug with low solubility and high permeability. This exerts rate-limiting effect on drug bioavailability. Objective: Improve the solubility/dissolution rate of asenapine maleate and hence the bioavailability using cocrystal approach. Method: Co-crystals were prepared using the solvent evaporation technique. Since the drug has H-bond acceptor count of 6, and H-bond donor count of 2, several co-formers were investigated. The co-crystals were evaluated using PXRD, FTIR spectroscopy, and DSC. Additionally, in-vitro dissolution studies were conducted. Results: The preparation of the co-crystals was successful. The PXRD patterns showed that the resultant mixture was crystalline, the FTIR confirmed the formation of H-bond between the drug and the co-formers and the DSC showed that the mixture exhibited a lower melting point as compared to the components and it was followed immediately by an exothermic peak, which confirmed the formation of co-crystals. The dissolution of all the prepared co-crystals using different co-formers in different ratios was much enhanced as compared to the unprocessed drug. The dissolution of the drug in the drug-nicotinamide co-crystals was much faster than that from the other co-crystals during the first 15-20 minutes. The dissolution of the drug from the physical mixture was slower than from the co-crystals during the first 15-20 minutes but the cumulative amount released after 120 minutes was almost the same. Conclusion: Co-crystals were prepared successfully by improving the solubility/dissolution rate of asenapine maleate, and were expected to enhance the bioavailability of the drug.

scholarly journals Solid Dispersions as a Technological Strategy to Improve the Bio-Performance of Antiparasitic Drugs with Limited Solubility

Proceedings ◽  
2020 ◽  
Vol 78 (1) ◽  
pp. 13
Author(s):  
Santiago N. Campos ◽  
Alicia G. Cid ◽  
Analía I. Romero ◽  
Mercedes Villegas ◽  
Cintia A. Briones Nieva ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Parasitic Infections ◽  
Dissolution Tests ◽  
Antiparasitic Drugs ◽  
Dissolution Efficiency ◽  
Time Required ◽  
Low Solubility ◽  
Initial Dissolution Rate

Albendazole (ABZ) and benznidazole (BZL) are drugs with low solubility used in parasitic infections treatment. In this research, solid dispersion (SD) technology was used to enhance ABZ and BZL performance by increasing their dissolution rate and solubility. SDs were prepared by the fusion method, employing Poloxamer 407 (P407) as carrier to disperse 32 of BZL or 50% w/w of ABZ. Furthermore, physical mixtures (PM) of P407 and either ABZ or BZL were also prepared, and then SDs and PMs were characterized. Dissolution tests of SDs, PMs and commercial formulations (CF) of ABZ and BZL were carried out and dissolution profiles were analyzed with the lumped mathematical model, which allowed parameters of pharmaceutical relevance to be obtained. The results indicated that ABZ SD presented an initial dissolution rate (IDR) 21-fold and 11-fold faster than PM and CF, respectively, while the IDR of BZL SD was 2.5-fold and 4.5-fold faster than PM and CF, respectively. For BZL formulations, the time required to reach 80% dissolution of the drug (t80%) was 4 (SD), 46 (PM), and 239 min (CF), while the dissolution efficiency (DE) at 30 min was 85 (DS), 71 (MF) and 65% (FC). For ABZ formulations, t80% was 2 (SD), value not reached (PM) and 40 min (CF), while the DE at 30 min was 85 (SD), 36 (MF) and 65% (CF). The SDs developed notably increased the dissolution rate, in consonance with the values obtained from the pharmaceutical parameters, which could lead to faster absorption and, consequently, increase the bioavailability of these drugs.

scholarly journals KARAKTERISASI FISIKOKIMIA NANOKRISTAL EKSTRAK HERBA SELEDRI ( Apium graveolens L.) DENGAN PERBEDAAN KONSENTRASI POLOXAMER188

2020 ◽  
Vol 4 (1) ◽  
pp. 31-39
Author(s):  
Henni Rosaini ◽  
Rina Wahyuni ◽  
Boyke Panata Sinaga ◽  
Wahyu Margi Sidoretno
Keyword(s):  
Particle Size ◽  
Apium Graveolens ◽  
Poloxamer 188 ◽  
Marker Compound ◽  
Biopharmaceutics Classification System Class ◽  
Particle Size Analyzer ◽  
Ft Ir ◽  
Low Solubility ◽  
Grinding Time

Celery (Apium graveolens L) is a plant of Apiaceae family which contains flavonoids, saponins, tannins, essential oils, apiin, apigenin, choline, asparagine, vitamin A, B, C. Apigenin contained in celery included in the BCS (Biopharmaceutics Classification System)  class II, which has low solubility and high permeability drugs. One method for increasing solubility is the nanocrystal method. Where the purpose of this study was to see the effect of differences in the concentration of poloxamer 188 on the characterization of nanocrystal. The results of the particle size analyzer (PSA) showed particle size distribution in formula 1 the concentration of poloxamer 188 40% 6 hour grinding time of 1648.5 nm with a potential zeta value of -11.2. While the formula 2 concentration of poloxamer 188 50% and formula 3 the concentration of poloxamer 188 60% with a 5 hour grinding time of 1049.6 and 1483.2 with a potential zeta value of -12.5 and -8.9. From the FT-IR analysis shows the presence of clusters in formulas 1, 2, and 3 which are not found in apigenin which is a celery marker compound, on the contrary there are groups on apigenin which are not found in formulas 1, 2, and 3.

scholarly journals Review: Effect of Different Methods on the Multicomponents Crystal Formation from Medicinal Natural Ingredient Compounds

2021 ◽  
Vol 6 (5) ◽  
pp. 32-39
Author(s):  
Eldya Nurismi ◽  
Henni Rosaini ◽  
dan Maria Dona Octavia
Keyword(s):  
Dissolution Rate ◽  
Classification System ◽  
Solvent Evaporation ◽  
Biopharmaceutics Classification System ◽  
Crystal Formation ◽  
High Permeability ◽  
Dissolution Rates ◽  
Solubility In Water ◽  
Low Solubility ◽  
Biopharmaceutics Classification

Solubility is an important parameter for the bioavailability of drugs that are difficult to dissolve. Natural compounds that are included in class II in the Biopharmaceutics Classification System (BCS) are Apigenin, Quercetin, Genistein, Curcumin, and Piperin. These drugs have low solubility in water and high permeability so that they affect the dissolution rate and as well as their bioavailability, to increase the solubility they are made with multicomponent crystals. This review aims to provide information on the method of making crystal multicomponent to increase the solubility and dissolution rate of BCS II drugs. Several methods that can be used in multicomponent are solvent drop grinding, solvent evaporation, assisted grinding, and slurry. The results showed that multicomponent crystals using several methods could increase the solubility and dissolution rates.

scholarly journals FORMULATION DEVELOPMENT AND CHARACTERIZATION OF TRIAMCINOLONE LOADED CUBOSOMES FOR TRANSDERMAL DRUG DELIVERY

2021 ◽  
Vol 6 (12) ◽  
pp. 1-17
Author(s):  
C. Pandian ◽  
A.Abdul Hasan Sathali ◽  
G. Abirami ◽  
E. Krithika
Keyword(s):  
Transdermal Delivery ◽  
In Vitro Release ◽  
Poloxamer 407 ◽  
Formulation Development ◽  
Inflammatory Reactions ◽  
Barrier Effects ◽  
Low Solubility

Psoriasis is a chronic condition that is caused by the negative signals given by immune system, which leads to hyperproliferation and other inflammatory reactions on the skin. These conditions may adversely affect the quality of the patient’s life leading to psychological stress. Topical delivery of drug is always preferred for Psoriasis because other treatments may lead to systemic intoxication and other adverse reactions. Triamcinolone is a topical corticosteroid belonging to BCS class IV (low solubility and permeability) used to treat Psoriasis. The limitations with transdermal delivery is that only a small amount of the drug can be transferred through the skin tissue due to the barrier effects of the Stratum corneum. Therefore, Novel transdermal delivery system, Cubosomes belonging to Nanostructured lipid carriers were chosen to overcome the issues of solubility and permeability. Twelve formulations were prepared with various ratios of Glyceryl monooleate (2.5 to 5%) & Poloxamer 407 (0.5 to 2%) and the formulations were evaluated for particle size, PDI, zeta potential, entrapment efficacy, drug content and in-vitro release. The best composition of Cubosomes was selected and incorporated into transdermal patch and the formulated patches were evaluated.

scholarly journals Preparation and Characterization of Nimesulide Nanoparticles For Dissolution Improvement

2018 ◽  
pp. 46-60
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Precipitation Method ◽  
Scanning Calorimetry ◽  
Decrease Particle Size ◽  
Antisolvent Precipitation ◽  
Particle Size Analyzer ◽  
Particle Size Increase ◽  
Freeze Dried ◽  
Inflammatory Drugs

Nimesulide is one of the types of non-steroidal anti-inflammatory drugs, widely used as analgesic and antipyretic. It is classified as class II drugs according to BCS guidance because of low solubility in water that leads to decrease in dissolution rate. So, the objective of this study was to decrease particle size, increase solubility and dissolution rate of nimesulide by preparation of nimesulide nanoparticles using solvent/antisolvent precipitation method by addition of organic solution of drug onto the solution of stabilizer. The size of nimesulide nanoparticles were studied and considered by particle size analyzer, drug content and loading efficiency. The freeze-dried nanoparticles were characterized by field emission electron microscope, X-Ray powder diffraction, differential scanning calorimetry and saturated solubility measurement. Tablet was manufactured by direct compression. The tablets were evaluated for drug release to measure the effect of nanoparticles on the dissolution improvement of drug.

Preparation and Characterization of Gossypol Nanosuspensions

2014 ◽  
Vol 1015 ◽  
pp. 713-720
Author(s):  
Si Tao Yang ◽  
Hui Tang ◽  
Yan Fang Liu ◽  
Xue Ying
Keyword(s):  
Particle Size ◽  
Physicochemical Characteristics ◽  
Water Soluble ◽  
Glycol Succinate ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Stabilizing Agents ◽  
Saturation Solubility ◽  
Freeze Dried

Gossypol (GP) is a kind of poorly water-soluble polyphenolic compounds. In this study, freeze dried gossypol nanosuspensions (GP-NS) were prepared by high-pressure homogenization and Freeze-drying technique. Bovine serum albumin (BSA) and D-alpha-tocopheryl polyethylene glycol succinate (TPGS) were used as stabilizing agents for the nanosuspensions while mannitol were used as lyophilized protecting medium. The physicochemical characteristics of the GP-NS were investigated when it was found that the mean particle size and zeta potential of the GP-NS were 217±23 nm and-21.4±2.7 mV, respectively, and the saturation solubility was 586.48±23.03 μg.mL-1. Differential scanning calorimetry and X-Ray Diffraction indicated that GP was in a crystalline state in nanosuspensions. GP-NS with a small particle size, and high saturation solubility, can be produced by the method described in this study.

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