scholarly journals DEVELOPMENT AND CHARACTERIZATION OF SUSTAINED RELEASE METHOTREXATE LOADED CUBOSOMES FOR TOPICAL DELIVERY IN RHEUMATOID ARTHRITIS

2020 ◽  
pp. 33-39
Author(s):  
KARISHMA KAPOOR ◽  
VINAY PANDIT ◽  
UPENDRA NAGAICH
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Poloxamer 407

Objective: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are essential part of the administration of Rheumatoid Arthritis (RA). Methotrexate (MTX) is effective for tumor necrosis factor alpha (TNF-a) biologic agents, indicated only in minority of patients suffering from severe RA. MTX remains the "anchor drug" in the treatment of RA. For delivery improvement, novel pharmaceutical drug delivery system i.e. MTX-Cubosomes were developed. Methods: Poloxamer 407 and Glycerol monooleate (Monoelin, MO) used and the formulation were characterized as a sustained release drug delivery system for Methotrexate. Different ratios of Monolein, Poloxamer 407 and water were used to develop the different cubosomes using homogenization and emulsification method. Characterization of formulations for morphology was performed and also particle size distribution by Transmission Electron Microscopy (TEM). Results: Formulation showed the internal cubic structures of the vesicles. The particle size of the formulations was found to be ranging from 53.21 to 185.32 nm, zeta potential of the formulations varied from-18.20-36.10 mV. The cubosomal formulation exhibited good entrapment efficiency along with high drug loading. Compatibility with the excipients was also established. An in vitro release study was done using Franz Diffusion cell indicated sustained release of the formulation at a rate of 1.25 %/h. Cubosomes proved to be reliable system for sustained transdermal drug delivery system. Conclusion: Methotrexate cubosomes is a novel medication delivery framework and in this examination it has been developed and characterized. The formulations were found to be promising in terms of its characterization parameters like particle size, zeta potential, entrapment efficiency, loading capacity, release kinetics, and stability, suitable for topical delivery.

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF FORMULATION SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM ETHANOL EXTRACT OF ROMANG PARANG LEAVES (BOEHMERIA VIRGATA)

2021 ◽  
pp. 207-212
Author(s):  
MAGFIRAH ◽  
INDAH KURNIA UTAMI
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Secondary Metabolites ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
Ethanol Extract ◽  
Polydispersity Index ◽  
Lattice Design

Objective: Parang romang (Boehmeria virgata) is one of the traditional medicines that are used empirically by Makassar tribal healers, South Sulawesi, as an antitumor drug. This traditional medicine contains secondary metabolites such as alkaloids, flavonoids, tannins, and saponins. However, secondary metabolites of those leaves extract have low solubility in water. Hence, to be formula, self-nanoemulsifying drug delivery system (SNEDDS) is one of the solutions to increase the extract solubility. Methods: The optimization of two formula optimum SNEDDS parang romang leaves (T80PGMZ and T20PGMZ) was using the simple lattice design (SLD) method which will give 28 SNEDDS formula parang romang leaves each of which the formula is tested for its characteristics as a critical point include emulsification time, % transmittance, drug loading, particle size, zeta potential, polydispersity index, and morphology particle. Results: The results of SNEDDS characterization obtained the optimum formula T80PGMZ with emulsification time 12.6 s, % transmittance 92.21%, drug loading 68.21 ppm, particle size 370.26 nm, zeta potential −31.4 mV, polydispersity index of 0.615, and regular particle morphology with spherical chunks at a magnification of 10,000 times with a particle size of 10 μm. Conclusion: SNEDDS of parang romang leaves extracts that used olive oil as oil phase, Tween 80 as a surfactant, and propylene glycol as the cosurfactant provided nanoemulsion with good characteristics.

Floating Microsphere of Curcumin as Targeted Gastro-retentive Drug Delivery System

2021 ◽  
pp. 5202-5206
Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Drug Bioavailability ◽  
Gastric Residence Time

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.

scholarly journals PHYSICOCHEMICAL CHARACTERIZATION OF PROPRANOLOL-LOADED CHITOSAN NANOPARTICLES FOR A BUCCAL DRUG DELIVERY SYSTEM

2020 ◽  
pp. 243-247
Author(s):  
SIRIPORN KITTIWISUT ◽  
PAKORN KRAISIT
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Chitosan Nanoparticles ◽  
Particle Sizes ◽  
Zeta Potentials ◽  
Ph Values ◽  
Buccal Drug Delivery

Objective: This study aimed to characterize the physicochemical properties, including pH, zeta potential, and particle size of propranolol-loaded nanoparticles that were incorporated into a buccal transmucosal drug-delivery system. Methods: An ionotropic gelation technique was used to formulate propranolol-loaded chitosan nanoparticles. Chitosan used as the nanoparticle base, using tripolyphosphate (TPP) as a cross-linking agent. The effects on nanoparticle physical properties, including pH, zeta potential, and particle size were examined when various chitosan [0.150-0.300 % (w/v)] and propranolol contents (0-40 mg) were used during the preparation. The effects of using chitosan solutions with different pH values on nanoparticle properties were also determined. Results: The pH values of all nanoparticles ranged between 4.14–4.55. The zeta potentials of the prepared nanoparticles ranged between 22.6–52.6 mV, with positive charges. The nanoparticle sizes ranged from 107–140 nm, which are within the range of suitable particle sizes for transmucosal preparations. Conclusion: The pH values, zeta potentials, and particle sizes of the nanoparticle formulations were influenced by the concentrations of chitosan and propranolol and by the pH of the initial chitosan solution. The relationships between nanoparticle properties and all factors primarily depended on the ionic charges of the components, especially chitosan. Our study provides beneficial physicochemical knowledge for the further development of chitosan-based nanoparticles containing propranolol for buccal drug delivery systems.

scholarly journals Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

2021 ◽  
Author(s):  
Cheran K ◽  
Udaykumar B Bolmal ◽  
Archana S Patil ◽  
Umashri A Kokatanur ◽  
Rajashree S Masareddy
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Gastro Retentive

Abstract Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.

scholarly journals Optimization of Self-Micro Emulsifying Drug Delivery System) for Soursop Leaf (Annona muricata Linn.) Chloroform Extract

2020 ◽  
Vol 25 (2) ◽  
pp. 81
Author(s):  
Anif Nur Artanti ◽  
Fea Prihapsara ◽  
Dian Eka Ermawati ◽  
Aprilia Saefanan Shofa
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Statistical Analysis ◽  
Zeta Potential ◽  
Propylene Glycol ◽  
Drug Delivery System ◽  
Delivery System ◽  
Tween 80 ◽  
Chloroform Extract ◽  
T Test

Soursop leaf chloroform extract has anticancer activity.  The active ingredient of soursop leaf was acetogenin polypoid derivatives that have a lipophilic characteristic, and less effective to achieve action targets of drugs in biological systems. The Self-Micro Emulsifying Drug Delivery System (SMEDDS) was an effective drug delivery technique that increases the solubility of lipophilic drugs. This study aims to determine the proportion of optimum SMEDDS formula using Simplex Lattice Design (SLD) method. The Formula of SMEDDS was prepared using a combination of Tween 80-Croduret, Propylene Glycol, and Candlenut oil. Optimization formula with SLD method using Design-Expert software based on physical stability parameters there are the percent of transmittance and emulsification time. The optimum formula of SMEDDS was compared with SLD prediction formula using a statistical analysis t-test, then test of loading dose extract, stability test accelerated by centrifugation, particle size, and zeta potential. The proportion of optimum composition of Tween 80-Croduret, Propylene Glycol, and Candlenut oil of SMEDDS was 60.87%; 24.13%; 15.00% respectively. Results of transmittance 41.14±3.78% and emulsification time 119.0±2.08 seconds. The predicted SLD value for the transmittance percent was 55.0% and the emulsification time was 119.59 seconds. The result of the statistical analysis of one sample t-test showed no significant difference between observation results and SLD prediction. The SMEDDS system has F value of 0.99 and capable to load 25.0 mg chloroform extract of soursop leaf each system with an average particle size of 440 nm and zeta potential of +21.5 mV. 

scholarly journals NANO-SPONGE NOVEL DRUG DELIVERY SYSTEM AS CARRIER OF ANTI-HYPERTENSIVE DRUG

2019 ◽  
pp. 47-63
Author(s):  
MONA IBRAHIM EL-ASSAL
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Concentration ◽  
Entrapment Efficiency ◽  
Plasma Drug Concentration ◽  
Production Yield ◽  
Pharmacokinetic Parameters ◽  
Plasma Drug

Objective: The study was designed to prepare Nano-sponge formulation loaded with nifedipine. Studying parameters which affecting the formulas in addition to pharmacokinetics and toxicity tests. Methods: Nine Nano-sponge formulations were prepared by the solvent evaporation technique. Different ratios of polymer ethylcellulose, CO-polymers β-cyclodextrin and hydroxypropyl β-cyclodextrin in addition to solubilizing agent polyvinyl alcohol were used. Thermal analysis, X-ray powder diffraction (XRPD), shape and surface morphology, particle size, %production yield, %porosity, % swelling, and % drug entrapment efficiency of Nano-sponge were examined. Release kinetic also studied beside comparison of pharmacokinetic parameters of the optimum choice formula and marketed one in addition to Toxicological consideration. Results: Particle size in the range of 119.1 nm to 529 nm which were increased due to the increase in the concentration of polymer to the drug. Nano-sponge revealed porous, spherical nature. Increased in the drug/polymer molar ratios (1:1 to 1:3) may increase their % production yield ranged from 62.1% to 92.4%. The drug content of different formulations was in the range of 77.9% to 94.7%, and entrapment efficiency was in the range of 82.72 % to 96.63%. Drug released in controlled sustained pattern and followed Higuchi, s diffusion mechanism. Pharmacokinetic parameters of optimized formula showed significant higher maximum plasma drug concentration, area under plasma concentration-time curve, volume of distribution and mean residence time. Nano-sponge loaded drug proved biological safety at low concentrations. Conclusion: Nano-sponge drug delivery system has showed small Nano size, porous with controlled drug release and significant-high plasma drug concentration that improved solubility, drug bioavailability and proved safety.

scholarly journals Novel combination for Self-nanoemulsifying Drug Delivery System of Candesartan Cilexetil

2018 ◽  
pp. 123-134
Author(s):  
Safa Fakher Mekhilef ◽  
Ahmed A. Hussein
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Water Solubility ◽  
Candesartan Cilexetil ◽  
Promising Result ◽  
Potential Measurement

Solubility problem of many of effective pharmaceutical molecules are still one of the major obstacle in theformulation of such molecules. Candesartan cilexetil (CC) is angiotensin II receptor antagonist with very low water solubility and this result in low and variable bioavailability. Self- emulsifying drug delivery system (SEDDS) showed promising result in overcoming solubility problem of many drug molecules. CC was prepared as SEDDS by using novel combination of two surfactants (tween 80 and cremophore EL) and tetraglycol as cosurfactant, in addition to the use of triacetin as oil. Different tests were performed in order to confirm the stability of the final product which includes thermodynamic study, determination of self-emulsification time, particle size and zeta potential measurement, and in-vitro drug release. The results showed that the particle size of the best formula was 13.3 nm and zeta potential of -37.45 mV with approximately 100% release after 45 minutes .These results suggest that the preparation of CC. as SEDDS with the use of the above combination of surfactant and cosurfactant is a promising maneuver for oral delivery of CC. in order to improve its bioavailability.   

Enhancement of Nimodipine Solubility by Self-Nano-emulsifying Drug Delivery System

2019 ◽  
Vol 12 (5) ◽  
pp. 4648-4656
Author(s):  
Suresh Gande ◽  
S. Srikanth Reddy ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Spherical Shape ◽  
Drug Dissolution ◽  
The Stability

Self-nanoemulsifying drug delivery system (SNEDDS) of Nimodipine was developed with the purpose of improving the bioavailability of the drug. Based on the results of Nimodipine solubility studies Peceol, Transcutol P and PEG 400 were optimized as oil, surfactant and co-surfactant for the formulation and Pseudo ternary plots was constructed by Chemix software. Fifteen formulations of Nimodipine SNEDDS prepared and analyzed for particle size, emulsification time, percentage drug release, percentage transmittance, in vitro drug dissolution studies and thermodynamic stability. The optimized Nimodipine SNEDDS formulation (F13) subjected to drug-excipient compatibility studies by FTIR. They are analyzed for zeta potential, SEM and stability. The particle size of optimized Nimodipine SNEDDS formulation was 25.9 nm, PDI is 0.382 and zeta potential -12.7 mV that are optimal for the stability of emulsion. SEM studies of Nimodipine SNEDDS indicated spherical shape and uniform particle distribution. The drug release of formulation F13 (98.25±4.77%) was higher than pure drug (38.49±3.88%). The stability studies indicated no change in drug content, drug release, emulsifying properties and appearance. Hence a potential SNEDDS formulation of Nimodipine developed with increased dissolution rate, bioavailability and solubility.

Formulation and Evaluation of Liposomal Drug Delivery System for Sulfasalazine

2021 ◽  
Vol 12 ◽  
Author(s):  
Sruthi P ◽  
Abbaraju Krishna Sailaja
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Good Stability ◽  
Folic Acid Deficiency ◽  
Liposomal Drug ◽  
Liposomal Drug Delivery

Aim: Aim of the current study is to prepare and characterize sulfasalazine-loaded liposomes to improve the bioavailability of the drug and to lessen the adverse effects of the drug. Background: Diseases like inflammatory bowel disease can be treated by anti-inflammatory agents like “Sulfasalazine,” It can also be used to treat ulcerative colitis and Crohn’s disease. The biological half-life of sulfasalazine is 5-10hr; as in the case of conventional therapy, there is a chance of missing the dose. Therefore, frequent administration of drugs is essential to maintain the desired steady-state level. The side effects are thrombocytopenia, megaloblastic anemia, bone marrow depression, folic acid deficiency, impairment of male fertility (Oligospermia), intestinal nephritis due to 5-ASA, diarrhoea, headache, and skin rashes. The bioavailability of sulfasalazine is 15%. This work was undertaken to enhance bioavailability and decrease the side effects. Objective: The main objective of the study is to improve the solubility of sulfasalazine by formulating a liposomal drug delivery system. The major objective is to develop a liposomal formulation with good stability and the highest entrapment efficiency. Methods: Liposomes were produced by the thin-film hydration method. Nine formulations of liposomes were prepared by varying the concentrations of soya lecithin and cholesterol and changing the drug ratio. The obtained liposomes were characterized for surface morphology, FTIR, particle size, zeta potential, drug content, entrapment efficiency, and in-vitro diffusion studies. Results: Among the nine formulations of liposomes, F3 was found to be the best formulation with an entrapment efficiency of 97.8% and a zeta potential value of -37.2mV. Liposomes followed first-order kinetics with a non-fickian diffusion pathway. Conclusions: Sulfasalazine loaded liposomes were prepared with good stability and the highest entrapment efficiency.

scholarly journals PREPARATION AND CHARACTERIZATION OF ETODOLAC BEARING EMULSOMES

2020 ◽  
pp. 166-172
Author(s):  
VIVEK GILL ◽  
ARUN NANDA
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Sustained Release ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Phospholipid Ratio ◽  
Predicted Values ◽  
Experimental Values

Objective: Emulsomes are novel vesicular drug delivery system with an internal solid lipid core surrounded by one or more bilayers of phospholipids. Etodolac is a potent anti-inflammatory drug and is a drug of choice for the treatment of various diseases. The present study is focused on the development of emulsomes using etodolac as drug candidates having improved drug loading with sustained-release effect for patient compliance. Methods: Emulsomes formulation composed of solid lipids (tristearin), phospholipids, cholesterol, stearylamine, and drug (etodolac) were prepared by lipid film hydration method followed by sonication to produce emulsomes of the nanometric size range. All the formulations were optimized by using box-behnken design of experiment considering 3 factors viz. drug to phospholipid ratio (A), tristearin to phospholipid ratio (B), stearylamine to phospholipid ratio (C) at 3 levels lower (-1), middle (0) and upper (+1). The response of the independent variables (A, B, C) was studied on the dependent variable viz. particle size (Y1), zeta potential (Y2), and entrapment efficiency (Y3). The responses were analyzed by design expert software to find out the optimized values of variables within the design space. Results: Compatibility with excipients was established by FTIR studies. The developed emulsomes were spherical shape vesicles as analyzed by TEM. The optimized batch (OB) was evaluated for particle size, zeta potential, and entrapment efficiency with experimental values 383.1 ± 11.7 nm, 47.2 ± 1.3 mV and 80.1 ± 3.2% and predicted values 390.394 nm, 45.000 mV and 81.642 %, respectively. The experimental values were found in reasonable agreement with predicted values by the design of the experiment. In vitro drug release study showed sustained release of the drug (88.69 % after 24 h). Conclusion: Etodolac loaded emulsomes is a novel drug delivery system and found to reliable in terms of various characteristic parameters like particle size, zeta potential, entrapment efficiency, and drug release. 3-factors 3-levels Box-behnken design of the experiment is a suitable design for the optimization of emulsomes.

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