scholarly journals Self Nano-Emulsifying Drug Delivery System (SNEDDS) of Curcuma Mangga Val. Essential Oil and The Stability Study

2020 ◽  
pp. 238-243
Author(s):  
Retno Sunarminingsih Sudibyo ◽  
Lukman Mahdi ◽  
Ronny Martien
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Essential Oil ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Droplet Size ◽  
Delivery System ◽  
Stability Study ◽  
Freeze Thaw ◽  
Lattice Design

Essential oil of Curcuma mangga Val. has been reported to have cytotoxic effect against cancer cell lines. But this oil is unstable in dispensing so that a self nano-emulsifying drug delivery system (SNEDDS) of the oil was conducted to solve the problem and improve its potency. In the study, optimization, verification, characterization, and stability test of the SNEDDS formula were carried out respectively by simplex lattice design (SLD) on Design Expert ver. 10 software, droplet size and Zeta potential determinations using particle size analyzer (PSA) instrument, as well as heating-cooling and freeze-thaw methods. The best SNEDDS formula resulted was Miglyol : Tween 80 : PEG 400 = 16.034% : 68.380% : 15.586%; with transmittance of 84.47 + 1.05%, droplet size of 15.75 nm, zeta potential of -8.54 mV, polydispersity index (PDI) of 0.188, emulsifying time of 49.67 + 1.7 seconds in distilled water, 24.33 + 4.19 seconds in artificial gastric fluid and 21.33 + 2.87 seconds in artificial intestine fluid. After a freeze-thaw test there was no change on the emulsion’s clarity, color, smell, as well as no separation, which means that the formula was stable thermodynamically. The optimum SNEDDS formula resulted has small particle size, better emulsifying time in artificial gastric and intestine fluids, as well as better thermodynamic stability, which in turn will improve the cytotoxic activity of the Curcuma mangga Val. rhizome oil toward cancer cells.

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.

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 MSc. Development of the In-house Specifications and Study of the Stability of Self-nanoemulsifying Drug Delivery System Containing Rosuvastatin

2020 ◽  
Vol 36 (4) ◽  
Author(s):  
Phan Thi Nghia ◽  
Tran Thi Hai Yen ◽  
Vu Thi Thu Giang
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Droplet Size ◽  
Delivery System ◽  
Clinical Medicine ◽  
Entrapment Efficiency ◽  
Clinical Effectiveness ◽  
Stability Study ◽  
Formulation Development ◽  
The Stability

This study develops the in-house specifications of self-nanoemulsifying drug delivery system (SNEDDS) containing rosuvastatin based on the following criteria: description, identification, droplet size (≤200 nm) and polydiversity index (not more than 0.3), drug proportion in the oil phase (≥ 90.0%), assay (≥ 95.0% and ≤105.0% of the labeled amount of rosuvastatin (C22H28FN3O6S). The criteria were validated and the results were suitable for identification and determination of rosuvastatin in SNEDDS. Additionally, the results of the stability study show that the rosuvastatin SNEDDS met the criteria of description, droplet size, PDI, assay and drug rate in the oil phase for 12-month storage under the long-term condition (12 months) and 6 months on accelerated condition. Keywords Rosuvastatin, SNEDDS, specification, droplet size, entrapment efficiency. References [1] A. Luvai, W. Mbagaya, A.S. Hall, I.H. Barth, Rosuvastatin: A Review of the Pharmacology and Clinical Effectiveness in Cardiovascular Disease, Clinical Medicine Insights: Cardiology 6 (2012) 17–33. https://doi.org/10.4137/CMC.S4324. [2] K. Balakumar, C.V. Raghavan, N.T. Selvan, R.H. Prasad, S. Abdu, Self nanoemulsifying drug delivery system (SNEDDS) of Rosuvastatin calcium: Design, formulation, bioavailability and pharmacokinetic evaluation, Colloids and Surfaces B: Biointerfaces. 112 (2013) 337–343. http://dx.doi.org/10.1016/j.colsurfb.2013.08.025. [3] S. Elkadi, S. Elsamaligy, S. Al-Suwayeh, H. Mahmoud, The Development of Self-nanoemulsifying Liquisolid Tablets to Improve the Dissolution of Simvastatin, American Association of Pharmaceutical Scientists 18(7) (2017) 2586–2597. https://doi.org/10.1208/s12249-017-0743-z. [4] D. Patel, K.K. Sawant, Self Micro-Emulsifying Drug Delivery System: Formulation Development and Biopharmaceutical Evaluation of Lipophilic Drugs, Current Drug Delivery 6 (2009) 419–424. https://doi.org/10.2174/156720109789000519. [5] S.D. Maurya, R.K.K. Arya, G Rajpal, R.C. Dhakar, Self-micro emulsifying drug delivery systems (SMEDDS): A review on physico-chemical and biopharmaceutical aspects, Journal of Drug Delivery and Therapeutics 7(3) (2017) 55–65. https://doi.org/10.22270/jddt.v7i3.1453.[6] P. Borman, D. Elder, Q2(R1) Validation of analytical procedures: text and methodology, in: A. Teasdale, D. Elder, R.W. Nims (Eds), ICH quality guidelines: an implementation guide, John Wiley & Sons Inc., Hoboken, 2018, pp. 127-166. [7] United States Pharmacopoeia 41, rosuvastatin tablets monograph.          

scholarly journals Vegetable Oil-Based Self-Microemulsifying Drug Delivery System of Eprosartan Mesylate: in vitro and ex vivo Evaluation

2021 ◽  
Vol 33 (9) ◽  
pp. 2182-2190
Author(s):  
Sabitri Bindhani ◽  
Snehamayee Mohapatra ◽  
Rajat Kumar Kar
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Ex Vivo ◽  
Tween 80 ◽  
Stability Study ◽  
Potent Drug

This study was planned to increase the intestinal permeability and thereby bioavailability of eprosartan mesylate (EPM) by designing a self-microemulsifying drug delivery system (SMEDDS) by the use of vegetable oils. Various SMEDDS-based formulations were prepared with oleic acid and peppermint oil. Tween 80 was used as surfactant and PEG 400 as co-surfactant. Pseudo ternary phase diagrams were constructed for identifying emulsification region between 1:1, 1:2, 2:1, 3:1 ratio of SCOS mix. Eight batches of SMEDDS were found to be thermodynamically stable and from which SMEDDSOF9 and PF5 were best formulations due to their highest drug content, minimum particle size. They have shown highest release of drug in vitro and higher in vitro drug diffusion and ex vivo permeation analysis than pure drug. FTIR study ascertained no incompatibility between drug and excipients present in formulation. From the accelerated stability study, slight effect on particle size and zeta potential, assay content along with cumulative % of drug release was found. The results demonstrated the SMEDDS of EPM are potent drug delivery system to increase dissolution rate and bioavailability of drug via increased intestinal permeability and consequently improving the therapeutic efficacy of eprosartan mesylate.

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 Preparation, characterization and antimicrobial activity of chitosan microparticles with thyme essential oil

2014 ◽  
Vol 68 (6) ◽  
pp. 721-729 ◽  
Author(s):  
Danijela Pecarski ◽  
Zorica Knezevic-Jugovic ◽  
Suzana Dimitrijevic-Brankovic ◽  
Katarina Mihajilovski ◽  
Slobodan Jankovic
Keyword(s):  
Drug Delivery ◽  
Antimicrobial Activity ◽  
Particle Size ◽  
Essential Oil ◽  
Essential Oils ◽  
Drug Delivery System ◽  
Delivery System ◽  
Thyme Oil ◽  
Chitosan Microparticles ◽  
Thyme Essential Oil

Considering the therapeutic effects of formulations with violate essential oils, development of an available drug delivery system is of great interest, especially assuming the fact that using essential oils as antimicrobial agents is a rather expanded in antimicrobial therapy nowadays. In this work, chitosan microparticles with encapsulated thyme essential oil were prepared by the emulsion cross-linking method. The effect of thyme oil and glutaraldehyde initial concentrations on particle size, morphology, and particle size distribution was investigated. In addition, the influence of these parameters on the encapsulation of thyme oil in chitosan microparticles, concerning thyme oil loadings and encapsulation efficiency was also tested. The particles showed a spherical shape with an average diameter from 4.71?1.42 to 13.65?4.34 m, depending on the concentration of the essential oil and glutaraldehyde that were used. The diameter of microparticles appeared to increase with increasing the thyme essential oil concentration, and decreased with the increase of glutaraldehyde concentration. It was shown that the concentration of glutaraldehyde did not affect the degree of encapsulation, but the increase in the initial concentration of thyme oil increased the degree of encapsulation of this essential oil in chitosan microparticles. All particles containing thyme essential oil, as well as essential oil of thyme itself showed significant antimicrobial activity against Staphylococcus aureus ATCC 25923, Esherichia coli ATCC 25922, Candida albicans ATCC 24433, Enterococcus faecalis ATCC 25929. This study showed a great potential of the use of thyme essential oil as an antimicrobial agent, especially when encapsulated in a drug delivery system with controlled release of the active antimicrobial component.

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.   

scholarly journals PREPARATION, CHARACTERIZATION AND STABILITY STUDIES OF SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM OF NIFEDIPINE

2020 ◽  
pp. 94-102
Author(s):  
SABITRI BINDHANI ◽  
SNEHAMAYEE MOHAPATRA ◽  
RAJAT KUMAR KAR
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Linseed Oil ◽  
Stability Study ◽  
In Vitro Dissolution

Objective: The objective of this work was to improve the solubility and dissolution rate of Nifedipine by preparing a solid-self micro emulsifying drug delivery system (Solid-smedds). Methods: Liquid-self-emulsifying drug delivery system formulations were prepared by using linseed oil as oil, tween 80 as a surfactant and PEG 400 as cosurfactant. Components were selected by solubility screening studies and the self-emulsifying region was identified by the pseudo-ternary phase diagram. Thermodynamic stability study was performed for the determination of stable liquid-smedds formulation. These formulations were evaluated for self-emulsification time, drug content analysis, robustness to dilution test, particle size analysis, in vitro diffusion study, and Stability study. Solid self-micro emulsifying formulations were prepared by using aerosil-200 at a different ratio. Lf9S (0.65:1) was selected due to its highest drug entrapment efficiency and a decrease in particle size. It was selected for further studies into DSC, SEM, FTIR, and XRD analysis. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM study, it was observed that the drug has been uniformly distributed and having a smooth surface. From the in vitro dissolution study, it improved the dissolution rate of nifedipine which was 98.70% of drug release where pure drug release only 6.72%. Conclusion: In conclusion, a solid self-micro emulsifying drug delivery system is improved the solubility and drug release rate but also improved the stability of the formulation.

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.

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.

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