scholarly journals The Effect of Drug Heterogeneous Distributions within Core-Sheath Nanostructures on Its Sustained Release Profiles

Biomolecules ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 1330 ◽  
Author(s):  
Haixia Xu ◽  
Xizi Xu ◽  
Siyu Li ◽  
Wen-Liang Song ◽  
Deng-Guang Yu ◽  
...  
Keyword(s):  
Sustained Release ◽  
Extended Release ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
The Core ◽  
Water Soluble Drug ◽  
Time Period ◽  
Drug Sustained Release ◽  
Water Soluble Drugs ◽  
Model Drug

The sustained release of a water-soluble drug is always a key and important issue in pharmaceutics. In this study, using cellulose acetate (CA) as a biomacromolecular matrix, core-sheath nanofibers were developed for providing a sustained release of a model drug—metformin hydrochloride (MET). The core–sheath nanofibers were fabricated using modified tri-axial electrospinning, in which a detachable homemade spinneret was explored. A process—nanostructure–performance relationship was demonstrated through a series of characterizations. The prepared nanofibers F2 could release 95% of the loaded MET through a time period of 23.4 h and had no initial burst effect. The successful sustained release performances of MET can be attributed to the following factors: (1) the reasonable application of insoluble CA as the filament-forming carrier, which determined that the drug was released through a diffusion manner; (2) the core–sheath nanostructure provided the possibility of both encapsulating the drug completely and realizing the heterogeneous distributions of MET in the nanofibers with a higher drug load core than the sheath; (3) the thickness of the sheath sections were able to be exploited for further manipulating a better drug extended release performance. The mechanisms for manipulating the drug sustained release behaviors are proposed. The present proof-of-concept protocols can pave a new way to develop many novel biomolecule-based nanostructures for extending the release of water-soluble drugs.

scholarly journals Calcium Chloride Modified Alginate Microparticles Formulated by the Spray Drying Process: A Strategy to Prolong the Release of Freely Soluble Drugs

Materials ◽  
2018 ◽  
Vol 11 (9) ◽  
pp. 1522 ◽  
Author(s):  
Marta Szekalska ◽  
Katarzyna Sosnowska ◽  
Anna Czajkowska-Kośnik ◽  
Katarzyna Winnicka
Keyword(s):  
Spray Drying ◽  
Drug Loading ◽  
Water Soluble ◽  
Cross Linking ◽  
Metformin Hydrochloride ◽  
Drying Process ◽  
Process Modification ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
One Step

Alginate (ALG) cross-linking by CaCl2 is a promising strategy to obtain modified-release drug delivery systems with mucoadhesive properties. However, current technologies to produce CaCl2 cross-linked alginate microparticles possess major disadvantages, such as a poor encapsulation efficiency of water-soluble drugs and a difficulty in controlling the process. Hence, this study presents a novel method that streamlines microparticle production by spray drying; a rapid, continuous, reproducible, and scalable technique enabling obtainment of a product with low moisture content, high drug loading, and a high production yield. To model a freely water-soluble drug, metformin hydrochloride (MF) was selected. It was observed that MF was successfully encapsulated in alginate microparticles cross-linked by CaCl2 using a one-step drying process. Modification of ALG provided drug release prolongation—particles obtained from 2% ALG cross-linked by 0.1% CaCl2 with a prolonged MF rate of dissolution of up to 12 h. Cross-linking of the ALG microparticles structure by CaCl2 decreased the swelling ratio and improved the mucoadhesive properties which were evaluated using porcine stomach mucosa.

scholarly journals Electrospun 4th-Generation Solid Dispersions of Poorly Water-Soluble Drug Utilizing Two Different Processes

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Zhu Zhang ◽  
Wenbing Li ◽  
Guanghua Wang ◽  
Yang-Lu Qu ◽  
Deng-Guang Yu
Keyword(s):  
Sustained Release ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Drug Sustained Release ◽  
Water Soluble Drugs ◽  
Effective Delivery ◽  
Polyethylene Glycol 1000 ◽  
Poorly Water Soluble

Different from traditional solid dispersion (SD) for improving the dissolution rates of poorly water-soluble drugs, the upgraded 4th SD was developed to furnish a drug sustained-release profile. In this work, two different kinds of 4th SDs were fabricated using two electrospinning processes. One is a ternary SD (nanofibers F2) that consisted of ethyl cellulose (EC), polyethylene glycol 1000 (PEG), and tamoxifen citrate (TAM) from a modified coaxial process, and the other is a binary SD (nanofibers F1) which is comprised of EC and TAM from a single-fluid blending process. Scanning electronic microscopic observations demonstrated that F2 (330±50 nm) showed a better quality than F1 (870±230 nm) in terms of size and size distribution although both of them had a smooth surface morphology and a cross section. X-ray diffraction patterns verified that both SDs were amorphous nanocomposites owing to the favorable secondary interactions among these components, as suggested from the results of FTIR. In vitro dissolution experiments indicated that F2 could furnish an improved drug sustained-release characteristics compared to F1, exhausting all the contained TAM and having weaker leveling-off late release. The molecular behaviors of drug sustained-release from the binary 4th SD were suggested. The protocols reported here paved an alternative way for developing novel functional nanomaterials for effective delivery of poorly water-soluble drugs.

scholarly journals DEVELOPMENT OF NATURAL AND MODIFIED GUM BASED SUSTAINED-RELEASE FILM-COATED TABLETS CONTAINING POORLY WATER-SOLUBLE DRUG

2019 ◽  
pp. 266-271
Author(s):  
AJAY KUMAR SHUKLA ◽  
RAM SINGH BISHNOI ◽  
MANISH KUMAR ◽  
C.P. JAIN
Keyword(s):  
Sustained Release ◽  
Release Rate ◽  
In Vitro Release ◽  
Release Profile ◽  
Water Soluble ◽  
The Core ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Seed Gum ◽  
Poorly Water Soluble Drug

Objective: The objective of this work was to the development of natural and modified gum based sustained-release film-coated tablets containing poorly water-soluble drug. Methods: Tamarind seed gum (TSG), fenugreek seed gum (FSG), sodium trimetaphosphate, hydroxypropyl methylcellulose (HPMC), sodium alginate (SA), and nifedipine (NFD) were used. The core tablets of nifedipine were prepared and evaluated for weight, diameters, thickness, hardness, and disintegration time. The core tablets were coated using 2% w/v solution of TSG, MTSG, FSG, and MFSG. The in vitro release rate of drug from these coated tablets was compared with the release rate of drug from the tablets coated with 2% w/v of HPMC. Results: The tablets coated with natural and modified TSG sustained the release of the drug up to 11 h and 14 h, respectively, and natural and modified FSG sustained release the drug up to 9 h and 11 h, respectively. The tablets coated with HPMC sustained released the drug up to 15 h. The drug release profile of tablets coated with modified TSG was comparable to the release profile of tablets coated with HPMC. Conclusion: On the basis of the release profile, it is concluded that unmodified and modified TSG can be used as release rate-controlling membrane.

scholarly journals Osmotic drug delivery system of valsartan

2019 ◽  
Vol 1 (2) ◽  
pp. 43-52
Author(s):  
Syed mujtaba pasha ◽  
Syed abid ali ◽  
Omair sohail ahmed ◽  
Omer wasiq ◽  
Mohammed mukaram ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Rate ◽  
Water Soluble ◽  
Hydrophilic Polymers ◽  
The Core ◽  
Drug Molecules ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Amitriptyline Hydrochloride

The objective of this study is to design and evaluate a new EOP called swellable elementary osmotic pump (SEOP) of the freely water soluble drug, amitriptyline hydrochloride (1 g /mL) by adding water swellable polymers in the core. The hydrophilic polymers included in the core retard the highly water soluble drug by producing hydrogel within the core, which may restrict and delay the solvent contact with drug molecules and may increase the diffusional length of the solvent to achieve a constant release rate. Thus, this technology can be exploited to achieve constant drug release at predetermined rate especially for highly water soluble drugs.

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques

2015 ◽  
Vol 8 (4) ◽  
pp. 3053-3059
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
H G Sandip
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Water Soluble ◽  
Wet Granulation ◽  
Wetting Properties ◽  
Enhanced Dissolution ◽  
Water Soluble Drug ◽  
Drug Concentrations ◽  
Water Soluble Drugs ◽  
Liquisolid Compacts

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.  

Polymer‐surfactant nanoparticles for sustained release of water‐soluble drugs

2007 ◽  
Vol 96 (12) ◽  
pp. 3379-3389 ◽  
Author(s):  
Mahesh D. Chavanpatil ◽  
Ayman Khdair ◽  
Yogesh Patil ◽  
Hitesh Handa ◽  
Guangzhao Mao ◽  
...  
Keyword(s):  
Sustained Release ◽  
Water Soluble ◽  
Water Soluble Drugs ◽  
Polymer Surfactant

Formulation development and characterization of highly water-soluble drug-loaded extended-release pellets prepared by extrusion–spheronization technique

2019 ◽  
Vol 16 (5) ◽  
pp. 1351-1365
Author(s):  
Muhammad Iqbal Nasiri ◽  
Rabia Ismail Yousuf ◽  
Muhammad Harris Shoaib ◽  
Kamran Zaheer ◽  
Tariq Ali ◽  
...  
Keyword(s):  
Extended Release ◽  
Water Soluble ◽  
Formulation Development ◽  
Water Soluble Drug ◽  
Extrusion Spheronization

scholarly journals Dissolution study of Spironolactone by using solid dispersion technique

2012 ◽  
Vol 4 (2) ◽  
pp. 42-47
Author(s):  
Irwin Dewan ◽  
SM Ashraful Islam ◽  
Mohammad Shahriar
Keyword(s):  
Drug Delivery ◽  
Solid Dispersion ◽  
Release Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dispersion Technique

The main objective of the current study was to formulate poorly water soluble drug Spirinolactone by using solid dispersion technique in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. Solid dispersions were prepared using two methods; solvent method and fusion method. Solid dispersion was prepared by using polymers, such as Hydroxy propylymethyl cellulose (HPMC 6cp), Hydroxy propyl cellulose (HPC), Sodium carboxymethylcellulose (Na-CMC), Povidone K12, Povidone K30, Poloxamer 407. Solid dispersions containing Spironolactone with HPC (96.81%), HPMC 6cp (93.05%), Poloxamer 407 (90.84%) and Na-CMC (89.93%) provided higher release rate than the release rate of solid dispersion containing only Spironolactone (35.27%), and Spironolactone with Povidone K12 (76.17%), Povidone K30 (67.92%). So the present study revealed that the solid dispersion may be an ideal means of drug delivery system for poorly water soluble drugs. Further study in this field was required to establish these drug delivery systems so that in future it can be used effectively in commercial basis.DOI: http://dx.doi.org/10.3329/sjps.v4i2.7776S. J. Pharm. Sci. 4(2) 2011: 42-47

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