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 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.    

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.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Development of an Innovative, Carrier-Based Dry Powder Inhalation Formulation Containing Spray-Dried Meloxicam Potassium to Improve the In Vitro and In Silico Aerodynamic Properties

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 535 ◽  
Author(s):  
Edit Benke ◽  
Árpád Farkas ◽  
Piroska Szabó-Révész ◽  
Rita Ambrus
Keyword(s):  
In Silico ◽  
Chronic Obstructive ◽  
Dry Powder Inhalation ◽  
Dry Powder ◽  
Aerodynamic Properties ◽  
Drug Concentrations ◽  
Anti Inflammatory ◽  
New Formulation ◽  
Spray Dried

Most of the marketed dry powder inhalation (DPI) products are traditional, carrier-based formulations with low drug concentrations deposited in the lung. However, due to their advantageous properties, their development has become justified. In our present work, we developed an innovative, carrier-based DPI system, which is an interactive physical blend of a surface-modified carrier and a spray-dried drug with suitable shape and size for pulmonary application. Meloxicam potassium, a nonsteroidal anti-inflammatory drug (NSAID), was used as an active ingredient due to its local anti-inflammatory effect and ability to decrease the progression of cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). The results of the in vitro and in silico investigations showed high lung deposition in the case of this new formulation, confirming that the interparticle interactions were changed favorably.

scholarly journals Inhalable Spray-Dried Chondroitin Sulphate Microparticles: Effect of Different Solvents on Particle Properties and Drug Activity

Polymers ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 425 ◽  
Author(s):  
Susana Rodrigues ◽  
Ana da Costa ◽  
Noelia Flórez-Fernández ◽  
María Torres ◽  
Maria Faleiro ◽  
...  
Keyword(s):  
Spray Drying ◽  
Chondroitin Sulphate ◽  
Antitubercular Activity ◽  
Particle Fraction ◽  
First Line ◽  
Antitubercular Drugs ◽  
Particle Properties ◽  
Aerodynamic Properties ◽  
Tuberculosis Therapy ◽  
Spray Dried

Spray-drying stands as one of the most used techniques to produce inhalable microparticles, but several parameters from both the process and the used materials affect the properties of the resulting microparticles. In this work, we describe the production of drug-loaded chondroitin sulphate microparticles by spray-drying, testing the effect of using different solvents during the process. Full characterisation of the polymer and of the aerodynamic properties of the obtained microparticles are provided envisaging an application in inhalable tuberculosis therapy. The spray-dried microparticles successfully associated two first-line antitubercular drugs (isoniazid and rifabutin) with satisfactory production yield (up to 85%) and drug association efficiency (60%–95%). Ethanol and HCl were tested as co-solvents to aid the solubilisation of rifabutin and microparticles produced with the former generally revealed the best features, presenting a better ability to sustainably release rifabutin. Moreover, these presented aerodynamic properties compatible with deep lung deposition, with an aerodynamic diameter around 4 μm and fine particle fraction of approximately 44%. Finally, it was further demonstrated that the antitubercular activity of the drugs remained unchanged after encapsulation independently of the used solvent.

scholarly journals PREPARATION, CHARACTERIZATION AND DISSOLUTION STUDY OF SPRAY DRIED SOLID DISPERSIONS OF SIMVASTATIN WITH PVP K25 AND AEROSIL 200

2021 ◽  
Vol 10 (6) ◽  
pp. 3806-3812
Author(s):  
Pritam Singh
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Drying Method ◽  
Bcs Class Ii ◽  
Enhanced Dissolution ◽  
Amorphous Nature ◽  
Characterization Studies

BCS class II is well-known for the drugs, having poor aqueous solubility and high permeability. Simvastatin is also categorized as BCS class II, suffering from poor aqueous solubility, affecting its bioavailability. In an attempt to resolve this problem, solid dispersions of simvastatin were prepared by spray-drying method. Solid dispersions of simvastatin with PVP K25 and aerosol in ratio (1:1:1 to 1:5:1) and without aerosil 200 (1:1 to 1:5) were prepared by spray drying method. The dissolution test showed the enhancement of dissolution as compared to the pure drug and nearly equal to marketed formulation “SIMVOTIN 20mg” in both types of formulation, but formulations with aerosil 200 showed faster drug release as compared to the simple formulations without aerosil. The formulation containing the 1:3:1 (simvastatin: PVP K25: Aerosil 200) showed the faster drug release as compared to other formulation that do not contain the Aerosil 200. Other characterization studies were also performed such as FTIR, differential scanning colorimetry and powdered X-ray crystallographic studies. These studies showed the increased amorphous nature of the drug in the formulation, which explain the enhanced dissolution rate of the drug for these formulations.

scholarly journals Development and Optimization of Proniosomal Gel Containing Etodolac: In-vitro, Ex-vivo and In-vivo Evaluation

2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
In Vivo Evaluation ◽  
Vesicle Size ◽  
Skin Delivery ◽  
The Stability

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.

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.

scholarly journals Itraconazole Niosomes Drug Delivery System and Its Antimycotic Activity against Candida albicans

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Vijay D. Wagh ◽  
Onkar J. Deshmukh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Cholesterol Content ◽  
Vesicle Size ◽  
Cholesterol Ratio ◽  
Antimycotic Activity

Niosomes have potential applications in topical drug delivery system. The objective of the study was to formulate and evaluate the niosome of Itraconazole. Surfactant : cholesterol ratio and quantity of ethanol used were studied by applying factorial design. Formulated niosomes were evaluated for vesicle size, entrapment efficiency, drug release, skin permeation, and antimycotic activity. Vesicle size, entrapment efficiency, and drug release were markedly dependent on surfactant : cholesterol ratio and quantity of ethanol used. Permeation of the drug through the skin was affected by cholesterol content in formulation. Itraconazole niosome were having larger zone of inhibition than marketed formulation when activity was checked against C. albicans. Niosomes may be a promising carrier for topical delivery of Itraconazole especially due to their simple production.

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