scholarly journals Preparation and characterization of phospholipid stabilized nanoemulsions in small-scale

2019 ◽  
Author(s):  
Shila Gurung ◽  
Martin Holzer ◽  
Sabine Barnert ◽  
Rolf Schubert

AbstractPhospholipids have been used to prepare liposomes. The use of phospholipids to stabilize nanoemulsions may cause spontaneous formation of liposomes. The main objective of this study is to develop a method to prepare phospholipid stabilized nanoemulsions in small scale (< 1 mL) and to minimize the formation of liposomes.A combination of hand extrusion and detergent removal methods was used in this study. Extrusion through polycarbonate membranes was performed in two steps, firstly using membranes of 400 nm followed by 200 nm membranes as the second step. Sodium cholate was used as a detergent to solubilize the formed liposomes which was later removed via dialysis. Nanoemulsions were characterized by measuring their particle size, polydispersity index and zeta-potential using Photon Correlation Spectroscopy and Cryo-TEM pictures. The stability of nanoemulsion stored under refrigeration was also studied.Fifty-one extrusion cycles through polycarbonate membrane of 400 nm pore size followed by one-hundred fifty-three cycles through polycarbonate membrane of 200 nm produced nanoemulsions having particle size below 200 nm (diameter). The nanoemulsions were found to be homogenous as depicted by polydispersity index (PDI) value below 0.1. Similarly, the zeta-potential was measured to be above −30 mV which is sufficient to keep nanoemulsions stable for as long as 7 months when stored under refrigeration. The Cryo-TEM pictures revealed 30 mM to be an optimum concentration of sodium cholate to prepare homogenous nanoemulsions with negligible proportion of liposomes.It was concluded that this method could be established as a small scale method of preparing nanoemulsions which will not only reduce the cost of preparation but also the disposal cost of toxic chemicals used for functionalizing nanoemulsions for scientific research.

2021 ◽  
Author(s):  
Nooryza Martihandini ◽  
Silvia Surini ◽  
Anton Bahtiar

Background: Andrographolide is a phytoconstituent with anti-inflammatory activity, however, the compound’s poor oral bioavailability has hindered its effective formulation for oral administration. This study, therefore, aims to develop an ethosome for improving andrographolide penetration through the transdermal delivery system. Methods: This study developed 3 ethosome formulas with different andrographolide-phospholipid weight ratios (1:8, 1:9; 1:10), using the thin-layer dispersion-sonication method. Subsequently, the ethosomes were evaluated for particle size, polydispersity index, zeta potential, morphology, as well as entrapment efficiency, and incorporated into a gel dosage form. Subsequently, an in vitro penetration study was performed using Franz diffusion cells for 24 hours and the stability of the gels at 5 ± 2°C, 30 ± 2°C, and 40 ± 2°C, were studied for 3 months. Results: The results showed the optimal formula was E2, a 1:9 weight ratio formula of andrographolide and phospholipid. Based on the transmission electron micrograph, E2 possessed unilamellar, as well as spherical-shaped vesicles, and exhibited superior characteristics for transdermal delivery, with a particle size of 89.95 ± 0.75 nm, polydispersity index of 0.254 ± 0.020, a zeta potential of -39.3 ± 0.82 mV, and entrapment efficiency of 97.89 ± 0.02%. Furthermore, the cumulative andrographolide penetration and transdermal flux for the ethosomal gel of E2 (EG2) were 129.25 ± 4.66 µg/cm2 and 5.16 ± 0.10 µg/cm2/hours, respectively. All the ethosomal gel formulations exhibited improved penetration enhancement of andrographolide, compared to the nonethosomal formulations. Also, the andrographolide levels in the ethosomal and nonethosomal gels after 3 months ranged from 98.13 to 104.19%, 97.93 to 104.01%, and 97.23 to 102.26% at storage temperatures of 5 ± 2°C, 30 ± 2°C/RH 65% ± 5%, and 40 ± 2°C/RH 75% ± 5%, respectively. Conclusions: This study concluded that encapsulation into ethosome enhances andrographolide delivery through the skin.


2019 ◽  
Vol 7 (2) ◽  
pp. 6-10
Author(s):  
Muhammad Dzakwan ◽  
Eko Pramukantoro Ganet ◽  
Mauludin Rachmat ◽  
Saleh Wikarsa

Fisetin (3,3,4,7-tetrahydroxyflavone) is a natural antioxidant that has shown to posses anticancer, antioxidant and anti-inflammatory properties. However, the poor solubility leads to poor bioavailability and limits its development.The aim of the research is to investigate the effect of fisetin nanosuspension using a nanoprecipitation technique and additional stabilizers polysorbat 80, SLS, PVA and Eudragit on particle size average, polydispersity index and zeta potential.The suspensions of microcrystalline FIS were prepared by a nanoprecipitation technique with different proportion of stabilizers fixed. The nanosuspension produced was then characterized using Photon Correlation Spectroscopy (PCS) in  term of particle size distribution, polydispersity index, zeta potential and morphology nanosuspensiom (TEM). Result showed fisetin nanosuspension were successfully prepared by anti-solvent precipitation with additional stabilizer SLS and polysorbat 80. The nanosuspension containing polysorbat 80 showed smaller average particle size of 225.7 nm ± 1.31, a polydispersity index of 0.272 ±0.02 and zeta potential -39.3 ± 0.26 was obtained. Conclusion, FIS nanosuspension successfully prepared by nanoprecipitation tecnique with the polysorbate 80 as stabilizer and ethanol as solvent were spherical in shape..


2018 ◽  
Vol 62 (3) ◽  
pp. 323-335 ◽  
Author(s):  
Barış Şimşek ◽  
Gözde Ultav ◽  
Haluk Korucu ◽  
Ahmet Yartaşı

The stability of the graphene oxide dispersions is an important issue in the preparation of medicine, printed flexible electronics, 3D printers and conductive inks. In order to improve the stability; mean and standard deviation of particle size, polydispersity index, zeta potential and conductivity of graphene oxide dispersion were selected as the main stability properties. The improvement rate between the estimate and the optimal conditions were calculated for the mean and standard deviation of particle size, polydispersity index, zeta potential and conductivity as 264.0%, 1875.0%, 583.3%, 5.0% and 50.0%, respectively in terms of the GO quality characteristics. The improvement rate between the estimate and the optimal conditions were calculated for the mean and standard deviation of particle size, polydispersity index, zeta potential and conductivity as 42.7%, 79.7%, -5.0%, 9.9% and -86.7%, respectively in terms of the GO quality characteristics. The result show that TOPSIS based Taguchi optimization in this study is effective to improve the graphene oxide dispersion stability.


2020 ◽  
Vol 17 (1) ◽  
pp. 172-183
Author(s):  
Nandanwadkar Shrikrishna Madhukar Hema ◽  
Mastiholimath Vinayak Shivamurthy ◽  
Pulija Karunakar

Introduction: Capsaicin (8-methy-N-vanillyl-6-nonenamide), a potential analgesic derived from Capsicum annuum (Chili peppers), widely used from ancient times for its pharmacological activities such as anti-inflammatory, anti-oxidant and analgesic and provides relief from migraine and diabetes. But for obvious reasons, capsaicin cannot be administered directly. The present work was designed with a focus to comply with mandatory requirement in various pharmacopeias to know the actual content of API present in final formulations. The formulation (TS3) consisting of 3% lipid, with 4:6 ratio of the polymer and solvent, was found to be the optimized formulation, which gave the best evaluation with regard to the particle size (97.03±2.68) nm, polydispersity index (0.20±0.00), higher zeta potential (61.28±2.06) mv, morphological studies and highest drug entrapment efficiency (68.34±4.24)%. The prepared transferosome formulation was subjected to characterization by validated HP-TLC method consisting of N-Hexane: Tert- Iso-butyl-methyl ether in ratio (5:15) v/v. Linearity was performed in the range of 50-1500 ng/spot with LOD/LOQ 50 ng and 150 ng, with regression analysis (R) of 99.91%. Recovery analysis was performed at 3 different levels at 80, 100 and 120 with an average recovery of 106.97%, respectively. Till now, no analytical method has been reported, associated with the characterization of pharmaceutical nano-forms (Capsaicin), like transferosomes. Thus, the maiden validated HP-TLC method for concurrent analysis of capsaicin as API in nano-transferosome may be employed in process quality control of formulations containing the said API. Background: The irritability and adverse effects post application, leading to inflammation and neural pain at the site of administration of newly Capsaicin API and its chemical entities and marketed formulations are usually related to poor permeability, leading to drug complex reactions in the development phases or therapeutic failure along with the quantification of the same in blood plasma. However, advancement in drug formulations with the use of polymer: alcohol ratio and modernized analytical techniques for the quantification of Pharmaceutical APIs seems to be emerging and promising for overcoming pain and related inflammatory complications by formulating the APIs in Transferosome formulation with Validated HP-TLC technique being used as an effective economic and precise tool for quantitative analysis of APIs in their respective nano-forms. Objective: The study proposes a novel standardized method development and validation of pharmaceutical nanoforms with Capsaicin as API. Method: Capsaicin Transferosomes were formulated using Ultra probe sonication by utilizing different proportions of phospholipid 90G dissolved in a mixture of ethanol and propylene glycol. The formulation was subjected to Dynamic Light Scattering (DLS) technique for nano-particle analysis followed by characterization with respect to particle size, polydispersity index, zeta potential and entrapment efficiency. The morphological study of vesicles was determined using SEM and TEM. A Validated HP-TLC method for the identification and determination of Capsaicin in transferosomes formulation was performed as per the ICH guidelines. Results: The formulation gave the best evaluation for particle size (97.03±2.68) nm, polydispersity index (0.20±0.00), higher zeta potential (61.28±2.06) mv, morphological studies (SEM & TEM) and highest drug entrapment efficiency (68.34±4.24)%. DSC thermograms and FTIR spectral patterns confirmed no physical interaction by polymers with API. The prepared formulation was then characterized using HP-TLC method. The best resolution was found in NHexane: Tert-Isobutyl methyl ether in a ratio of 5:15 v/v. The Rf was found to be 0.3±0.03. Linearity was performed in a range of 50-1500 ng/spot, with regression analysis (R) of 99.91% Further, recovery analysis was done at 3 different levels as 80, 100 and 120 with an average recovery of 106.97%. The LOD/LOQ was found to be 50 and 150 ng, respectively. Precision was carried out in which % RSD was found to be precise and accurate. Conclusion: The outcomes of the present study suggested that the proposed novel formulation analyzed by Validated planar chromatographic technique (HP-TLC) for Capsaicin quantification in nanoforms may be employed as a routine quality control method for the said API in various other formulations.


Author(s):  
RISA AHDYANI ◽  
LARAS NOVITASARI ◽  
RONNY MARTIEN

Objective: The objectives of this study were to formulate and characterize nanoparticles gel of timolol maleate (TM) by ionic gelation method using chitosan (CS) and sodium alginate (SA). Methods: Optimization was carried out by factorial design using Design Expert®10.0.1 software to obtain the concentration of CS, SA, and calcium chloride (CaCl2) to produce the optimum formula of TM nanoparticles. The optimum formula was characterized for particle size, polydispersity index, entrapment efficiency, Zeta potential, and molecular structure. Hydroxy Propyl Methyl Cellulose (HPMC) K15 was incorporated into optimum formula to form nanoparticles gel of TM and carried out in vivo release study using the Franz Diffusion Cell. Results: TM nanoparticles was successfully prepared with concentration of CS, SA, and CaCl2 of 0.01 % (w/v), 0.1 % (w/v), and 0.25 % (w/v), respectively. The particle size, polydispersity index, entrapment efficiency, and Zeta potential were found to be 200.47±4.20 nm, 0.27±0.0154, 35.23±4.55 %, and-5.68±1.80 mV, respectively. The result of FTIR spectra indicated TM-loaded in the nanoparticles system. In vitro release profile of TM-loaded nanoparticles gel showed controlled release and the Korsmeyer-Peppas model was found to be the best fit for drug release kinetics. Conclusion: TM-loaded CS/SA nanoparticles gel was successfully prepared and could be considered as a promising candidate for controlled TM delivery of infantile hemangioma treatment.


2021 ◽  
Vol 901 ◽  
pp. 117-122
Author(s):  
Netnapa Ontao ◽  
Sirivan Athikomkulchai ◽  
Sarin Tadtong ◽  
Phuriwat Leesawat ◽  
Chuda Chittasupho

Ocimum gratissimum L. leaf oil exhibited many pharmacological properties. This study aimed to formulate and evaluate the physical and chemical stability of O.gratissimum leaf oil nanoemulsion. O.gratissimum leaf oil was extracted by hydrodistillation. The major component of the essential oil eugenol, was analyzed by UV-Vis spectrophotometry. Nanoemulsions of O.gratissimum leaf oil were formulated using polysorbate 80, hyaluronic acid, poloxamer 188, and deionized water by phase inversion composition method. The hydrodynamic diameter, polydispersity index, and zeta potential value of O.gratissimum leaf oil nanoemulsion was evaluated by a dynamic light scattering technique. The %remaining of eugenol in the nanoemulsion was analyzed by UV-Vis spectrophotometry. The essential oil extracted from of O. gratissimum leaf oil was a clear, pale yellow color. The %yield of the essential oil was 0.15 ± 0.03% v/w. The size of the nanoemulsion was less than 106 nm. The polydispersity index of the nanoemulsion was ranging from 0.303 - 0.586 and the zeta potential value of the nanoemulsion was closely to zero, depending on the formulation component. O. gratissimum leaf oil at concentrations ranging from 0.002 - 0.012% v/v contained 35 - 41% of eugenol. The size of nanoemulsion was significantly decreased after storage at 4 °C, while significantly increased upon storage at 45 °C. The size of nanoemulsion stored at 30 °C did not significantly change. The %remaining of eugenol in the nanoemulsion was more than 90% after storage at 4 °C and 30 °C for 28 days. The percentage of eugenol remaining in the nanoemulsion stored at 45 °C was more than 85 - 90%, suggesting that the temperature affected the stability of eugenol in the nanoemulsion.


Author(s):  
MAGFIRAH ◽  
INDAH KURNIA UTAMI

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.


Author(s):  
RADITYA ISWANDANA ◽  
RICHA NURSELVIANA ◽  
SUTRIYO SUTRIYO

Objective: Gold nanoparticles (AuNPs) are highly useful for drug delivery, but their application is limited by their stability as they readily aggregate.This issue can be prevented by adding a stabilizing agent such as resveratrol (RSV), which is a polyphenol derived from plants, that is used to preventcancer. Therefore, we propose a novel method to prepare stable RSV-conjugated nanoparticles modified with polyethylene glycol (RSV-AuNP-PEG).Methods: In the first step, the Turkevich method was used to synthesize the AuNPs. Then, PEG was added as stabilizer agent and conjugated with RSV.The synthesized conjugates were characterized using ultraviolet-visible spectrophotometry, Fourier transform infrared spectroscopy, particle sizeanalysis, and high-performance liquid chromatography.Results: The obtained RSV-AuNP-PEG had a particle size of 83.93 nm with a polydispersity index (PDI) of 0.562 and formed a translucent purple-redfluid in solution. The zeta potential was −22.9 mV, and the highest entrapment efficiency was 75.86±0.66%. For comparison, the RSV-AuNP solutionwas purple and turbid, the particle size was 51.97 nm with a PDI of 0.694, and the zeta potential was −24.6 mV. The stability test results showed thatthe storage stability of RSV-AuNP-PEG was better than that of AuNP-RSV. Further, the RSV-AuNP-PEG was shown to be most stable in 2% bovine serumalbumin (BSA) while the AuNP-RSV was most stable in 2% BSA in phosphate-buffered saline pH 7.4.Conclusion: These results show that modification of RSV-conjugated AuNPs with PEG effectively prevents their aggregation in storage, but only incertain mediums.


Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5632
Author(s):  
Weixuan Sun ◽  
Wenhan Yang ◽  
Yuxue Zheng ◽  
Huiling Zhang ◽  
Haitian Fang ◽  
...  

In order to broaden the application of potato pulp pectic polysaccharide (PPP) in stabilizing acidified milk drinks (AMDs) and investigate the stabilizing effect and physical properties of AMDs prepared with PPP, a comparative study was made among PPP, commercial high methoxyl pectin (HMP) and low methoxyl pectin (LMP). The zeta potential, rheology, particle size and serum separation of AMDs were evaluated after preparing with PPP, HMP and LMP, respectively. Results indicated that PPP led to lower serum separation than LMP (14.65% for AMDs prepared with 0.5% PPP compared to 25.05% for AMDs prepared with 0.5% LMP), but still higher than HMP (9.09% for AMDs prepared with 0.5% HMP). However, narrower particle size distribution and lower viscosity of AMDs was achieved by PPP than by LMP and HMP. PPP can electrostatically adsorb on the surface of casein and its abundant neutral sugar side chains would provide steric hindrance to prevent casein flocculation in AMDs. Our results might provide some new ideas for the application of PPP in improving the stability of AMDs.


2020 ◽  
Vol 1001 ◽  
pp. 110-114
Author(s):  
Xiao Qi Chen ◽  
Meng Meng Zhou ◽  
Zheng Zheng Wang ◽  
Hai Jun Zhou ◽  
Shu Lan Yang ◽  
...  

A series of oil in water (O/W) microemulsions were prepared through drop by drop method at constant temperature, taking Span80/Tween80 as a composite emulsifying system and Macol-52 as oil phase. Effects of the mass ratio of composite emulsifying system and oil/emulsifier ratio on the particle size were studied. Finally, the best technological conditions were selected and the stability of the microemulsion was also researched. Results showed that the most suitable Span80/Tween80 mass ratio was 1:1 and the oil/emulsifier ratio is 1:1. Under this condition, the mean particle size of the o/w microemulsion was 71.1 nm and the polydispersity index was 0.151. Moreover, the microemulsion maintain a bright and uniform stable system after 20minutes’ centrifugation at the speed of 4000r/min and the particle size increased slightly.


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