scholarly journals Formulation of Spray-dried Proliposomes Loaded with Berberin

2021 ◽  
Vol 37 (2) ◽  
Author(s):  
Tran Thi Hai Yen ◽  
Tran Thi Nhu Quynh ◽  
Duong Thi Thuan ◽  
Pham Thi Minh Hue
Keyword(s):  
Drug Delivery ◽  
Spray Drying ◽  
Entrapment Efficiency ◽  
Sodium Deoxycholate ◽  
Film Deposition ◽  
Migration And Invasion ◽  
Average Particle ◽  
Drying Method ◽  
Ethanol Injection ◽  
Spray Dried

The aims of study was formulation and evaluation of berberin (BBR) loaded proliposomes by spray-drying method. BBR proliposomes were evaluated for appearance, spray-drying efficiency, morphology and differential scanning calorimetry (DSC). Liposomes, obtained after hydration, were evaluated for particle size, size distribution, morphology and entrapment efficiency. The results showed that BBR proliposomes were prepared by spray-drying method with molar ratio of Hydrogenated soy phosphatidyl choline (HSPC): Sodium deoxycholat (NaDC): vitamin E (vtE): BBR = 7: 1: 6: 6. Mixture of manitol and Aerosil at weight ratio of 97:3 was used as carrier. Results of DSC showed that berberin was dispersed molecularly into proliposomes powder. BBR liposomes, obtained after hydration, had average particle diameter of about 29 μm and entrapment efficiency was 22.23%. Keywords Proliposomes, liposomes, berberin, sodium deoxycholate, spray-dried. References [1] W. Kong, J. Wei, A. Parrveen et al., Berberine is A Novel Cholesterol-Lowering Drug Working Through A Unique Mechanism Distinct From Statins, Nature Medicine, Vol. 10, No. 12, 2004, pp. 1344-1351, https://doi.org/10.1038/nm1135.[2] S. K. Kulkarni, A. Dhir, on The Mechanism of Antidepressant-Like Action of Berberine Chloride, European Journal of Pharmacology, Vol. 589, No. 1-3, 2008, pp. 163-172, https://doi.org/ 10.1016/j.ejphar.2008.05.043.[3] Y. T. Ho, J. S. Yang, T. C. Li et al., Berberine Suppresses in Vitro Migration and Invasion of Human SCC-4 Tongue Squamous Cancer Cells Through the Inhibitions of FAK, IKK, NF-Κb, U-PA and MMP-2 and-9, Cancer Letters, Vol. 279, No. 2, 2009, pp. 155-162, https://doi.org/10.1016/j.canlet.2009.01.033.[4] S. Muneer, Z. Masood, S. Butt et al., Proliposomes as Pharmaceutical Drug Delivery System: A Brief Review, Journal of Nanomedicine and Nanotechnology, Vol. 8, No. 3, 2017, pp. 448-450, https://doi.org/10.4172/2157-7439.1000448.[5] H. K. Omer, N. R. Hussein, A. Ferraz et al., Spray-Dried Proliposome Microparticles for High-Performance Aerosol Delivery Using a Monodose Powder Inhaler, AAPS PharmSciTech, Vol. 19, No. 5, 2018, pp. 2434-2448, https://doi.org/10.1208/s12249-018-1058-4.[6] T. T. H. Yen, T. T. N. Quynh, D. T. Thuan, P. T. M. Hue, Preparation of Berberin Liposomes, Contained Sodium Deoxycholate by Ethanol Injection Method, Journal of Pharmaceutical Research and Drug information, Vol. 11, No. 4, 2020, pp. 11-17 (in Vietnamese). [7] T. T. H. Yen, T. T. Hue, P. T. M. Hue et al., Preparation of Berberin Proliposomes by Film Deposition on Carrier Surface Method, VNU Journal of Science: Medical and Pharmaceutical Sciences, Vol. 36, No. 2, 2020, pp. 9-15, https://doi.org/10.25073/2588-1132/vnumps.4204.[8] R. G. Ahmed, S. Sherif, Z. Zainab et al., Silymarin Spray-Dried Proliposomes: Preparation, Characterization and Cytotoxic Evaluation, Drug Delivery Letters, Vol. 10, No. 1, 2020, pp. 14-23, https://doi.org/10.2174/2210303109666190722114211.[9] A. Bangham, M. M. Standish, J. C. Watkins Diffusion of Univalent Ions Across the Lamellae of Swollen Phospholipids, Journal of Molecular Biology, Vol. 13, No. 1, 1965, pp. 238-252.    

Inhalable Spray Dried Pro-Liposome Powder Containing Budesonide for Pulmonary Delivery

2021 ◽  
Vol 14 (4) ◽  
pp. 5538-5548
Author(s):  
Aliasgar J Kundawala ◽  
Khushbu S Chauhan ◽  
Harsha V Patel ◽  
Swati K Kurtkoti
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Entrapment Efficiency ◽  
Geometric Standard Deviation ◽  
Drying Method ◽  
Dry Powder ◽  
Liposomal Drug ◽  
Vesicle Size ◽  
Aerodynamic Properties ◽  
Spray Dried

Budesonide is an anti-asthmatic agent which is used to control the symptoms of asthma like bronchospasm, oedema. Drug delivered to lung through inhalation will provide systemic and local drug delivery at lower dose in chronic and acute diseases. Dry powder inhalers are the best choice for targeting the anti-asthmatic drugs through pulmonary route. The objective of the present study is to prepare inhalable lipid coated budesonide microparticles by spray drying method so effective delivery of budesonide to the lungs can be achieved. The microparticles in the form of dry powder were obtained by either spray drying liposomal drug suspension or lipid drug suspension. The liposomes were initially prepared by solvent evaporation method using Hydrogenated Soyabean Phosphatidylcholine and Cholesterol (1:1, 1:2, 2:1) as lipid carrier and then spray dried later with mannitol as bulking agent at different lipid to diluent ratio (1:1.25, 1:2.5 & 1:5). The liposomes and liposomal dry powder were evaluated for vesicle size, % entrapment efficiency, in vitro drug release studies, powder characteristics, aerosol performance and stability studies. The liposomes prepared showed vesicle size (2-8 µm), Entrapment efficiency (92.22%) at lipid: drug ratio of (2.5:1) and observed 80.41 % drug release in 24 hrs. Pro-liposomes prepared by spray drying of liposomal drug suspension (LSD1) showed emitted dose, mean mass aerodynamic diameter, geometric standard deviation and fine particle fraction of 99.01%, 3.12 µm, 1.78 and 43.5% along with good powder properties. The spray dried powder was found to be stable at 4 ± 2 °C & 65% ± 5 % RH. The inhalable microparticles containing Budesonide containing lipid dry powder was successfully prepared by spray drying method that showed good aerodynamic properties and stability with mannitol as diluent. The microparticles produced with this novel approach could deliver drug on target via inhalation route and also ease manufacture process at large scale in fewer production steps.

scholarly journals Physico-Chemical and In Vitro Characterization of Chitosan-Based Microspheres Intended for Nasal Administration

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 608
Author(s):  
Csilla Bartos ◽  
Patrícia Varga ◽  
Piroska Szabó-Révész ◽  
Rita Ambrus
Keyword(s):  
Drug Delivery ◽  
Spray Drying ◽  
Process Parameters ◽  
Sodium Tripolyphosphate ◽  
Structural Characteristics ◽  
Nasal Administration ◽  
Drug Bioavailability ◽  
Intranasal Application ◽  
Spray Dried

The absorption of non-steroidal anti-inflammatory drugs (NSAIDs) through the nasal epithelium offers an innovative opportunity in the field of pain therapy. Thanks to the bonding of chitosan to the nasal mucosa and its permeability-enhancing effect, it is an excellent choice to formulate microspheres for the increase of drug bioavailability. The aim of our work includes the preparation of spray-dried cross-linked and non-cross-linked chitosan-based drug delivery systems for intranasal application, the optimization of spray-drying process parameters (inlet air temperature, pump rate), and the composition of samples. Cross-linked products were prepared by using different amounts of sodium tripolyphosphate. On top of these, the micrometric properties, the structural characteristics, the in vitro drug release, and the in vitro permeability of the products were studied. Spray-drying resulted in micronized chitosan particles (2–4 μm) regardless of the process parameters. The meloxicam (MEL)-containing microspheres showed nearly spherical habit, while MEL was present in a molecularly dispersed state. The highest dissolved (>90%) and permeated (~45 µg/cm2) MEL amount was detected from the non-cross-linked sample. Our results indicate that spray-dried MEL-containing chitosan microparticles may be recommended for the development of a novel drug delivery system to decrease acute pain or enhance analgesia by intranasal application.

scholarly journals Preparation of LiFePO4 Powders by Ultrasonic Spray Drying Method and Their Memory Effect

Materials ◽  
2021 ◽  
Vol 14 (12) ◽  
pp. 3193
Author(s):  
Tu Lan ◽  
Xiaolong Guo ◽  
De Li ◽  
Yong Chen
Keyword(s):  
Spray Drying ◽  
Memory Effect ◽  
Electrode Materials ◽  
Average Particle Size ◽  
Lithium Ion ◽  
Average Particle ◽  
Preparation Process ◽  
Drying Method ◽  
Drying Temperature ◽  
Ultrasonic Spray

The memory effect of lithium-ion batteries (LIBs) was first discovered in LiFePO4, but its origin and dependence are still not clear, which is essential for regulating the memory effect. In this paper, a home-made spray drying device was used to successfully synthesize LiFePO4 with an average particle size of about 1 μm, and we studied the influence of spray drying temperature on the memory effect of LiFePO4 in LIBs. The results showed that the increasing of spray drying temperature made the memory effect of LiFePO4 strengthen from 1.3 mV to 2.9 mV, while the capacity decreased by approximately 6%. The XRD refinement and FTIR spectra indicate that the enhancement of memory effect can be attributed to the increment of Li–Fe dislocations. This work reveals the dependence of memory effect of LiFePO4 on spray drying temperature, which will guide us to optimize the preparation process of electrode materials and improve the management system of LIBs.

Preparation and pharmacokinetics of cefquinome sulfate liposomes in goats

2018 ◽  
Author(s):  
Haigang Wu ◽  
Jinni Liu ◽  
Gugangke Xu ◽  
Zhaowei Ye ◽  
Jicheng Liu and Benchi Yi
Keyword(s):  
Plasma Concentration ◽  
Particle Diameter ◽  
Entrapment Efficiency ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Average Particle ◽  
Average Particle Diameter ◽  
Ethanol Injection ◽  
Elimination Half ◽  
Time Point

We evaluated the pharmacokinetics of cefquinome sulfate (CEF) liposomes in eight healthy goats following intramuscular administration at 4 mg/kg. The average particle diameter of CEF liposomes prepared by the ethanol injection method was 335nm with a CEF entrapment efficiency of 69.56%. The elimination half-life (t1/2b) of CEF liposomes was 33.04h compared with 16.21 h for CEF injected without carrier (p less than 0.05). The area under the concentration curve (AUC) for CEF liposomes was approximately three-times greater than for CEF alone (P less than 0.05). The time-point of maximum plasma concentration of the drug (Tp) and the maximum plasma concentration (Cmax) were 4.38 h and 1.99 ìg/mL for CEF liposomes, compared with 1.86 h and 3.55 ìg/mL for CEF without carrier, respectively. 

The Morphology of Si-K-HAs Composite Prepared by Spray Drying

2019 ◽  
Vol 966 ◽  
pp. 19-24
Author(s):  
Srie Muljani ◽  
Heru Setyawan ◽  
Ketut Sumada
Keyword(s):  
Surface Area ◽  
Spray Drying ◽  
Humic Substance ◽  
Spherical Particles ◽  
Precipitation Method ◽  
Infrared Spectrometry ◽  
Drying Method ◽  
X Ray Diffraction ◽  
X Ray ◽  
Spray Dried

The silica potassium humic substance (Si-K-HAs) composite have been produce by spray drying successfully. In the previous study the preparation of Si-K-HAs gel by precipitation method required the addition of acid so that Si-K-HAs gel product contains acid salts. This study was develope spray drying method in order to eliminate the use of acid. The mixture of potassium silicate, cellulose and humic potassium solution was mixed with varying volume ratios and flowed into a spray dryer to produce Si-K-HAs powder. The used of cellulose (CMC) in this study acts as a homogeneous agent so that silica and humic substance can be completely mixed at controlled viscosity. Si-K-HAs products were characterized by Scanning electron microscopy (SEM), X-ray fluorescence (XRF), X-ray diffraction (XRD), Fourier transform infrared spectrometry (FTIR), and Surface area analytical (SAA). The result showed that the Si-K-HAs composite prepared by spray dryers have spherical particles, SiO2 in the range of 48-50%, K2O in the range of 49-50%. The present of cellulose caused the increasing of Si-K-HAs particle size e.g 17.30 μm prepared without CMC to 41.11 μm prepared with addition of 100g of CMC. The presence of cellulose can also increase the surface area of the spray-dried Si-K-HAs particles from 111.92 m2g-1; 163.241 m2g-1.

scholarly journals The Effect of Pharmaceutical Excipients for Applying to Spray-Dried Omega-3 Powder

2019 ◽  
Vol 9 (6) ◽  
pp. 1177 ◽  
Author(s):  
◽  
◽  
◽  
◽  
◽  
...  
Keyword(s):  
Fatty Acid ◽  
Solid State ◽  
Spray Drying ◽  
Human Body ◽  
Blood Clotting ◽  
Acid Oxidation ◽  
Omega 3 ◽  
Drying Method ◽  
Omega 3 Fatty Acid ◽  
Spray Dried

Omega-3 fatty acid plays a role in protecting cells in the human body, maintaining the structure of the cell, and helping smooth metabolism. Also, it inhibits the formation of blood clotting and is effective in enhancing the formation of bone. However, the instability due to fatty acid oxidation and a fishy smell are the reasons it is avoided by people. In this study, we tried to obtain the omega-3 powder through spray-drying method using a variety of binders and surfactants for improving the limit of omega-3 fatty acid. First of all, an olive oil was used instead of omega-3 for optimization of the preparation of spray-dried omega-3 powder. Through the screening of binders and surfactants, γ-cyclodextrin and hydrogenated lecithin were chosen as a binder and a surfactant, respectively. Omega-3-loaded spray-dried powder was obtained, eventually. The morphology of omega-3-loaded spray-dried powder was spherical of 310 nm and the DHA amount was 98%. This study suggested that the transformation of omega-3 fatty acid into solid state by spray-drying using a binder and a surfactant was successively performed.

Investigation on the Preparation, Characteristics, and Controlled Release Model of Paeonol-Loaded Liposome in Carbomer Hydrogel

2020 ◽  
Vol 17 (2) ◽  
pp. 159-173
Author(s):  
Qinqin Liu ◽  
Hongmei Xia ◽  
Yinxiang Xu ◽  
Yongfeng Cheng ◽  
Zhiqing Cheng
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Average Particle ◽  
Filtration Method ◽  
Ethanol Injection ◽  
Soybean Phospholipid ◽  
Release Model

Objective: Paeonol is a phenolic compounce that is volatile. In order to decrease its volatility and achieve controlled release, paeonol-loaded liposome in carbomer hydrogel was prepared by coating with soybean phospholipid via ethanol injection method and then added into the carbomer hydrogel. Methods: The quality of paeonol-loaded liposome in carbomer hydrogel was evaluated by the degree of roundness, particle size distribution, zeta potential, entrapment efficiency (filtration method and chitosan neutralization method), viscosity, infrared spectrum, etc. Furthermore, the diffusion from paeonolloaded liposome in hydrogel was studied in vitro. Results: The results showed that the average particle size of paeonol-loaded liposome was about 401 nm, the potential was -17.8 mV, and the entrapment efficiency was above 45%. The viscosity of paeonol- loaded liposome in hydrogel was 23.972×10-3 Pa*s, and the diffusion rate from paeonol-loaded liposome in hydrogel in vitro was obviously slower than that from the other paeonol preparations. Conclusion: The conclusions could be drawn that paeonol-loaded liposome in hydrogel was a kind of novel preparation, and its diffusion in vitro had obvious controlled-release characteristics, which further proved that it might improve the bioavailability of paeonol.

The effect of chitosan type and drug-chitosan ratio on physical characteristics and release profile of ketoprofen microparticles prepared by spray drying

2021 ◽  
Vol 32 (4) ◽  
pp. 669-673
Author(s):  
Muhammad A. S. Rijal ◽  
Hanah Masitah ◽  
Fanny Purvitasari ◽  
Retno Sari
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Release Rate ◽  
Entrapment Efficiency ◽  
Physical Characteristics ◽  
Release Profile ◽  
Efficiency Evaluation ◽  
Intestinal Fluid ◽  
Drying Method ◽  
Simulated Intestinal Fluid

Abstract Objectives In order to minimize gastrointestinal irritation and to extend the absorption of ketoprofen, microparticles prepared with chitosan have been developed. In this study, chitosan type and drug-chitosan ratio were investigated to prepare microparticles of ketoprofen and evaluated for physical characteristics and drug release profiles. Methods Microparticles were prepared by using ionic gelation methods with chitosan, which has two different viscosities i.e., 19 and 50 cPs, cross-linked with tripolyphosphate, and dried by spray drying method. The microparticles were made with a drug-chitosan ratio of 5:15 and 6:15. Results The results showed that the microparticles had spherical shapes. Increasing the amount of ketoprofen improved the drug content and entrapment efficiency. Evaluation of drug release in simulated intestinal fluid (pH 6.8) showed that the microparticles prepared with chitosan 19 cPs had the slowest release rate than those of chitosan 50 cPs, while that of the microparticles prepared with chitosan 50 cPs with the ratio of drug/polymer 6:15 was the fastest, as shown by its slope value. The release rate of microparticles with chitosan 19 cPs was slower than those microparticles with chitosan 50 cPs. Conclusions It could be suggested that by increasing the amount of ketoprofen, it improved the entrapment efficiency and the release rate of microparticles.

Effect of Nano Silicon Dioxide on Tablet Properties of Rice Starch

2010 ◽  
Vol 93-94 ◽  
pp. 679-682 ◽  
Author(s):  
Varatus Vongsurakrai ◽  
Saiyavit Varavinit
Keyword(s):  
Silicon Dioxide ◽  
Spray Drying ◽  
Rice Starch ◽  
Drying Method ◽  
Disintegration Time ◽  
Tablet Properties ◽  
Dry Mixing ◽  
Mixing Method ◽  
Frictional Forces ◽  
Spray Dried

Starch-colloidal silicon dioxide mixtures (Era-Tab SP® ) was prepared by co-spray drying and dry mixing methods and the flow ability and tablet properties of both methods were compared in particular with spray dried rice starch (SNR) alone. In co-spray drying, various percentages of rice starch and colloidal silicon dioxide blends were suspended in distilled water and subjected to spray dryer. The dry mixing method was obtained by blending of the colloidal silicon dioxide and spray dried rice starch at various percentages. It was found that co-spray drying of starch-colloidal silicon dioxide mixtures improved flow ability by reducing of the frictional forces between the granules greater than the dry mixing method. SEM micrographs presented the depositions of colloidal silicon dioxide on the surface of agglomerated starch granules obtained from both methods. The addition of colloidal silicon dioxide increased the tensile strength of the compressed tablet especially via the co-spray drying method by increasing the interaction of hydrogen bonding inside the tablet. Moreover, the co-spray drying method also reduced the friability and the disintegration time of the tablets better than the dry mixing method.

scholarly journals Physical Characteristics of Cilostazol–Hydroxybenzoic Acid Cocrystals Prepared Using a Spray Drying Method

Crystals ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 313
Author(s):  
Maho Urano ◽  
Megumi Kitahara ◽  
Kae Kishi ◽  
Eiichi Goto ◽  
Tatsuaki Tagami ◽  
...  
Keyword(s):  
Spray Drying ◽  
Drying Methods ◽  
Hydroxybenzoic Acid ◽  
Drying Method ◽  
Drying Process ◽  
Dihydroxybenzoic Acid ◽  
Drug Substances ◽  
Derivatives Of ◽  
As Solubility ◽  
Spray Dried

The cocrystal formation of pharmaceuticals can improve the various physical properties of drugs, such as solubility, without the need for chemical modification of the drug substances. In the present study, we prepared cocrystals of cilostazol and additive coformers (derivatives of hydroxybenzoic acid) using a spray drying method. Based on the preparation of the cocrystals of cilostazol and the coformers as reported previously, the characteristics of the cilostazol cocrystals prepared using solvent evaporation, slurry, and spray drying methods were compared. The physical characterization revealed that the spray drying method successfully produced cilostazol–4-hydroxybenzoic acid and cilostazol–2,4-dihydroxybenzoic acid cocrystals, whereas samples of cocrystals of cilostazol and 2,5-dihydroxybenzoic acid produced via the spray drying process appeared to contain coformer polymorphs. The dissolution of cilostazol was improved using the spray-dried cocrystal samples composed of coformers compared to samples prepared using cilostazol alone or a physical mixture. The present results provide useful information regarding the manufacture of cilostazol cocrystals and pharmaceutical cocrystals via spray drying in large-batch production.

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