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.

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 Preparation and characterization of azathioprine microspheres for colon specific delivery

2019 ◽  
Vol 9 (2) ◽  
pp. 97-101
Author(s):  
Rinku Gonekar ◽  
Mohan Lal Kori
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Study Drug ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Intestinal Fluid ◽  
Drug Release Profile ◽  
Fecal Matter

The objective of the present study is to develop colon targeted drug delivery system using dextrin (polysaccharide) as a carrier for Azathioprine.  Microspheres containing azathioprine, dextrin and various excipients were prepared by solvent evaporation technique. The prepared microsphere were evaluated by different methods parameters like particle size,  drug entrapment efficiency, percentage yield, shape and surface morphology  and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Best formulation was decided on the basis drug release profile in simulated gastric, intestinal fluid and simulated colonic fluid. In dextrin based microspheres, dextrin as a carrier was found to be suitable for targeting of Azathioprine for local action in the site of colon. Dextrin microspheres released 95-99% of azathioprine in simulated colonic fluid with 4% human fecal matter solution. The results of in-vitro studies of the azathioprine microspheres indicate that for colon targeting dextrin are suitable carriers to deliver the drug specifically in the colonic region. Dextrin based azathoprine microspheres showed no significance change in particle size and % residual upon storage at 5 ± 3ºC, 25 ± 2ºC/60 ± 5% RH (room temperature) and 40 ± 2ºC/75 ±5%RH humidity for three months. Keywords: azathioprine, microsphere, dextrin, colon specific drug delivery.

Development and Validation of UV-Visible Spectrophotometric method for the Estimation of Curcumin and Tetrahydrocurcumin in Simulated Intestinal Fluid

2021 ◽  
pp. 2971-2975
Author(s):  
Jai Bharti Sharma ◽  
Sherry Sherry ◽  
Shailendra Bhatt ◽  
Vipin Saini ◽  
Manish Kumar
Keyword(s):  
Drug Release ◽  
Spectrophotometric Method ◽  
Tween 80 ◽  
Solvent System ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Validation Parameters ◽  
Administration Method ◽  
Uv Visible ◽  
Development And Validation

Background: Due to solubility issues of curcumin and tetrahydrocurcumin, there is a need for the development of a UV-Visible spectrophotometric method that can estimate the drug release precisely and accurately. The addition of surfactant in the dissolution medium in low concentration achieved bio-comparable surface activity and can be used to estimate the drug release from formulations by avoiding sink conditions. Objective: The purpose of the present investigation was to develop a simple and précise UV-Visible spectrophotometric method for the determination of curcumin and tetrahydrocurcumin after oral administration. Method: A UV-Visible spectrophotometric method was developed using an appropriate solvent system for the estimation of curcumin and tetrahydrocurcumin. The solvent system having simulated intestinal fluid and particular concentration of surfactant was selected and further validated according to guidelines of the international conference on harmonization (ICH), the analytical parameter like linearity, precision and accuracy, etc. were studied. Results: Simulated intestinal fluid pH 7.4 with tween 80 at 1 % concentration satisfied all the conditions relative to peak quality at the stated wavelength for curcumin and intestinal fluid pH 7.4 with tween 80 at 0.5% concentration satisfied all the conditions relative to Peak quality at the stated wavelength for tetrahydrocurcumin. The developed methods were found within the range of all the validation parameters. Conclusion: The proposed method was found to be very simple and precise and can be used for routine quantitative analysis of curcumin and tetrahydrocurcumin.

scholarly journals Drug Release from a Spherical Matrix: Theoretical Analysis for a Finite Dissolution Rate Affected by Geometric Shape of Dispersed Drugs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 582
Author(s):  
Yung-Sheng Lin ◽  
Ruey-Yug Tsay
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Shape Factor ◽  
Numerical Solutions ◽  
Drug Loading ◽  
Spherical Geometry ◽  
Detailed Comparison ◽  
Release Profile ◽  
Drug Release Profile ◽  
Drug Release Rate

Amending the neglect of finite dissolution in traditional release models, this study proposed a more generalized drug release model considering the simultaneous dissolution and diffusion procedure from a drug-loaded spherical matrix. How the shape factor (n = 0, 1/2, and 2/3 for the planar, cylindrical, and spherical geometry, respectively) of dispersed drug particles affected the release from the matrix was examined for the first time. Numerical solutions of this generalized model were validated by consensus with a short-time analytical solution for planar drugs and by the approach of the diffusion-controlled limits with Higuchi’s model. The drug release rate increases with the ratio of dissolution/diffusion rate (G) and the ratio of solubility/drug loading (K) but decreases with the shape factor of drug particles. A zero-order release profile is identified for planar drugs before starting the surface depletion layer, and also found for cylindrical and spherical dispersed drugs when K and G are small, i.e. the loaded drug is mainly un-dissolved and the drug release rate is dissolution-controlled. It is also shown that for the case of a small G value, the variation of drug release profile, due to the drug particle geometry, becomes prominent. Detailed comparison with the results of the traditional Higuchi’s model indicates that Higuchi’s model can be applied only when G is large because of the assumption of an instantaneous dissolution. For K = 1/101–1/2, the present analysis suggests an error of 33–85% for drug release predicted by Higuchi’s model for G = 100, 14–44% error for G = 101, while a less than 5% error for G ≧ 103.

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.    

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.

Competition Between Heparin and Polyethylene Glycol as Biofunctionalization for Improving Stability of Liposomal Doxorubicin

2020 ◽  
Vol 12 (2) ◽  
pp. 271-277
Author(s):  
Eman R. Abbase ◽  
Medhat W. Shafaa ◽  
Mohsen M. Mady
Keyword(s):  
Polyethylene Glycol ◽  
Drug Release ◽  
Zeta Potential ◽  
Release Rate ◽  
Liposomal Doxorubicin ◽  
Entrapment Efficiency ◽  
Drug Release Rate ◽  
Pegylated Liposomes ◽  
Positively Charged ◽  
Mcf 7

In order to improve liposomal doxorubicin stability, differentiation between Heparin and Polyethylene Glycol (PEG) as biofunctionalization for liposomal doxorubicin has been investigated by measuring the entrapment efficiency, size distribution, zeta potential, evaluating the in vitro potential cytotoxicity against MCF-7 (Breast cancer cell) and stability in serum by measuring the drug release rate. We synthesized Four liposomal formulations: (A) Conventional liposomes; DPPC:DOX, (B) Positively charged PEGylated liposomes; DPPC:CHOL:SA:PEG:DOX (C) Negatively charged PEGylated liposomes: DPPC:CHOl:DCP:PEG:DOX (D) positively charged liposomes to conjugate heparin; DPPC:CHOL:SA:DOX. Entrapment efficiency of doxorubicin dramatically increased after PEGylation and conjugation with heparin. In addition, zeta potential was changed upon the encapsulation of doxorubicin into conventional and PEGylated liposomes which indicates that DOX encapsulated completely into liposomes. For heparin conjugated liposomes, zeta potential was slightly changed. Sulphorhodamine-B (SRB) assay showed a greater cytotoxic effect of the liposomal doxorubicin formulations at different concentrations with respect to free drug against MCF-7 cell lines. The anticancer activity order was observed between the various liposome formulations, especially those observed with conjugated heparin liposomes. Slower drug release rate showed an order of D > C > B > A that means stability showed an order of D > C > B > A. From above results, the most stable liposomal doxorubicin formulation was the liposomal formulation D. The results optimized using heparin than PEG as biofunctionalization. Further studies are suggested for better understanding why heparin improves the stability of liposomal doxorubicin.

scholarly journals Effect of Channeling Agents on the Release Profile of Theophylline from METHOCEL K4M Based Matrix tablets

1970 ◽  
Vol 7 (1) ◽  
pp. 27-32 ◽  
Author(s):  
Md Shaikhul Millat Ibn Razzak ◽  
Ferdous Khan ◽  
Md Ziaur Rahman Khan ◽  
Kanij Fatema ◽  
Muhammed Shahidul Islam ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Release Profile ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Release Mechanism ◽  
Dissolution Profile ◽  
Compression Process ◽  
Low Viscosity ◽  
Time Required

The present study was undertaken to investigate the effect of channeling agents on the release profile of Theophylline from METHOCEL K4M based matrix systems. Matrix tablets of Theophylline using METHOCEL K4M were prepared by direct compression process. METHOCEL K4M polymer is hydrophilic in nature. NaCl and PEG 1500 were used as channeling agents. Drug release study was evaluated for eight hours using USP 22 paddletype dissolution apparatus using distilled water as the dissolution medium. The release mechanisms were explored and explained with zero order, Higuchi and Korsmeyer equations. The release rate, extent and mechanisms were found to be governed by channeling agent type and content. Higher channeling agent content (42.49%) in the matrix increased the rate and extent of the drug release because of increased porosity in the tablet matrices, at lower channeling agent (19.76%) level, the rate and extent of drug release was decreased and in absence of channeling agents these were least. NaCl ensures maximum release of drug from low viscosity grade METHOCEL K4M than PEG 1500 when other parameters were kept constant. It was found that type and amount of channeling agent significantly affect the time required for 50% of drug release (T50%), percentage drug release at 8 hours, release rate constant (K) and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was mainly dependent on the presence of type and amount of channeling agent. These studies indicate that the proper balance between a matrix forming agent and a channeling agent can produce a drug dissolution profile similar to a theoretical dissolution profile.Key words: Channeling agent, Theophylline, Release Profile, Methocel K4MDOI = 10.3329/dujps.v7i1.1214Dhaka Univ. J. Pharm. Sci. 7(1): 27-32, 2008 (June)

scholarly journals Characterization and in vitro release study of artesunateloaded microparticles prepared using crosslinked-chitosan and its derivatives

2020 ◽  
Vol 19 (6) ◽  
pp. 1139-1146
Author(s):  
Retno Sari ◽  
Meta Dian Feriza ◽  
Amani Syarahil ◽  
Andang Miatmoko ◽  
Dwi Setyawan
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Crosslinking Agent ◽  
In Vitro Release ◽  
Flow Speed ◽  
Carboxymethyl Chitosan ◽  
Physical Characteristics ◽  
Drying Methods ◽  
Crosslinking Agents

Purpose: To determine the effect of crosslinking on the physical characteristics, recovery, and release of artesunate-loaded chitosan and carboxymethyl chitosan microparticles.Methods: The artesunate microparticles were prepared by means of ionic gelation-spray drying methods involving the use of a crosslinking agent i.e. tripolyphosphate for chitosan and CaCl2 for carboxymethyl chitosan. The drug-polymer solution mixture was introduced into the crosslinker solution and stirred for two hours at 500 rpm prior to drying at a temperature of 100ºC, a pressure of 2 mbar and a flow speed of 6.0 mL/min. The resulting microparticles were subsequently evaluated for their morphology, physical state, drug content and in vitro drug release.Results: The results showed that the type of chitosan and crosslinking affected particle shape, surface roughness, drug recovery, and drug release. The artesunate microparticles prepared with cross-linked polymer demonstrated a lower encapsulation efficiency due to the barriers presented by the crosslinking agents. The use of carboxymethyl chitosan increased the release rate of the artesunate from the microparticles by up to 1.2 times (16.78 mg/ml.min½), while chitosan decreased it 0.7 times (9.12 mg/ml.min½) compared to artesunate alone (13.54 mg/ml.min½).Conclusion: The use of crosslinking agents and chitosan type affects the physical characteristics of artesunate in addition to its release rate from microparticles. Keywords: Artesunate, Chitosan, Carboxymethyl chitosan, Crosslinking, Microparticle, Drug release

Design, Formulation and Characterization of Microspheres containing Mesalamine for the Treatment of Ulcerative Colitis

2021 ◽  
pp. 165-169
Author(s):  
Deepak Patel ◽  
Sunil Kumar Shah ◽  
Chandra Kishore Tyagi
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Simulated Gastric Fluid ◽  
Simulated Intestinal Fluid ◽  
Chitosan Microspheres ◽  
Increase With Increase

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72% - 82.27%, drug loading from 20.28% - 33.26%. The size of the prepared microspheres ranged between 61.22-90.41μm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. The release profile of mesalamine from eudragit-coated chitosan micro-spheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.

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