A Comparative Study of Acyclovir icroencapsulation by Novel Solvent Evaporation-Matrix Erosion and Spray Drying Techniques

2012 ◽  
Vol 5 (1) ◽  
pp. 1627-1637
Author(s):  
J P Raval ◽  
D R Naik
Keyword(s):  
Spray Drying ◽  
Ethyl Cellulose ◽  
Drug Loading ◽  
In Vitro Release ◽  
Spherical Geometry ◽  
Solvent Evaporation ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Spray Dried

Designing and evaluating a multiparticulate controlled release dosage form, to increase the efficacy of acyclovir (a selective antiherpes agent). Spray drying technique for microsphere production is compared with novel solvent evaporation-matrix erosion technique for variable drug loading in different concentration of ethyl cellulose. The microspheres were characterized for physicochemical properties. The microspheres sizes were ranged from 7-25 μm. The spray dried microspheres had better encapsulation efficiency (up to 91%) compared to that of novel solvent evaporation-matrix erosion technique microspheres. Scanning electron microscopy confirmed spherical geometry due to high cross-linking density. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and x-ray diffraction studies showed chemical stability and intactness of entrapped drug in the microspheres. In vitro release of acyclovir from spray dried microspheres continued for longer period compared to novel solvent evaporation-matrix erosion method. Overall, the release studies depended on the concentration of ethyl cellulose, extent of drug loading, and the technique used to prepare microspheres. Thus, marked retardation of drug release may provide a useful effective anti-retroviral drug therapy.  

scholarly journals Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

2020 ◽  
Vol 2020 ◽  
pp. 1-15
Author(s):  
Qiuchen Cheng ◽  
Wen Qin ◽  
Yanhong Yu ◽  
Guojian Li ◽  
Jizhou Wu ◽  
...  
Keyword(s):  
Smooth Muscle Actin ◽  
Drug Loading ◽  
In Vitro Release ◽  
Tween 80 ◽  
Original Method ◽  
Scanning Calorimetry ◽  
Experimental Conditions ◽  
Evaporation Method ◽  
Genistein Treatment

The objective of this study is to improve the bioavailability of genistein by encapsulation with polyethylene glycol-polylactic acid (PEG-PLA) copolymers. Genistein micelles (GMs) prepared using a modified emulsion-evaporation method were more stable than those made with the original method. The effect of polyvinyl alcohol, Tween 80, sonication time, PEG-PLA/genistein ratio, and organic phase (acetone)/H2O ratio on the size, polydispersity index, encapsulation efficiency, and drug loading efficiency of GMs was investigated. GMs were obtained and characterized under optimal experimental conditions. For long-term storage, GMs were lyophilized by freeze drying with trehalose to produce genistein lyophilized powder (GLP). The analysis of GLP by Fourier-transform infrared spectroscopy and differential scanning calorimetry showed that genistein was successfully incorporated into the micellar structure. In vitro release experiments revealed that the incorporation of genistein into PEG-PLA copolymers significantly improved its solubility and bioavailability. GLP was more potent in inhibiting the proliferation of HSC-T6 cells than genistein. Treatment with GLP at 10–20 μg/mL for 48 h significantly inhibited the protein expression of α-smooth muscle actin and collagen I in HSC-T6 cells compared with the control. These data demonstrated that the improved solubility and bioavailability of genistein in the form of GLP enhanced its antifibrotic effect in vitro.

Formulation and Evaluation of Fast Dissolving Gliclazide Tablets by Complexation with Hydroxypropyl-β-Cyclodextrin

2014 ◽  
Vol 7 (1) ◽  
pp. 2399-2405
Author(s):  
Adel M Aly ◽  
Khaled M. Al-Akhali ◽  
Hesham Alrefaey ◽  
Mahmoud A. Shaker
Keyword(s):  
Dissolution Rate ◽  
Spray Drying ◽  
Inclusion Complexes ◽  
In Vitro Release ◽  
Hypoglycemic Effect ◽  
Scanning Calorimetry ◽  
Molar Ratios ◽  
Market Product

Gliclazide (GZ) is practically insoluble in water and its bioavailability is limited by dissolution rate. The aim of the present study was to enhance the dissolution rate and bioavailability of GZ by complexation with hydroxypropyl (HP)-β-cyclodextrin (CD) applying three different methods; physical mixing, kneading technique and spray drying technique.  Also, to evaluate the dissolution rate and the hypoglycemic effect of the prepared complexes, in comparison with the GZ market product (Glizide tablets) in Saudi market. The produced complexes were characterized and evaluated using Differential Scanning Calorimetry (DSC), X-ray Diffractometry (XRD), Scanning Electron Microscope (SEM) and the in vitro release studies. All the methods of preparation of complexes were found to be effective in improving the solubility of gliclazide in comparison with the commercial product (Glizide tablets). The formation of inclusion complexes was evident in these formulations as shown by DSC and XRD studies. The inclusion complexes prepared by spray drying method in 1:1 molar ratios were the most effective method for improving the solubility of GZ. The in-vivo hypoglycemic effect of the complexed GZ-HP-β-CD prepared by spray drying significantly improved the biological performance and therapeutic efficacy of the drug compared to Glizide market product.  

Nanostructured-lipid carriers-Chitosan hydrogel beads carrier system for loading of resveratrol: A new method of topical application

2022 ◽  
pp. 088532822110539
Author(s):  
Bi Wu ◽  
Yang Li ◽  
Yuan Y Li ◽  
Zhi H Shi ◽  
Xiao H Bian ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Physical Stability ◽  
In Vitro Release ◽  
In Vitro Cytotoxicity ◽  
Nanostructured Lipid Carriers ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Chitosan Hydrogel ◽  
Hydrogel Beads

The aim of this study was to develop nanostructured-lipid carriers (NLC) encapsulated by Chitosan hydrogel beads for the efficient topical carrier. Dynamic light scattering (DLS), X-ray diffraction (XRD), Differential scanning calorimetry (DSC), and attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) were conducted to study the influence of the encapsulation on the characteristic of resveratrol-loaded NLC, and the results showed that there was no impact on resveratrol-loaded NLC. Chitosan hydrogel beads could significantly improve the physical stability of resveratrol-loaded NLC. In vitro release study revealed that resveratrol-loaded NLC-Chitosan hydrogel beads had a more significant sustained-release effect on resveratrol. In vitro transdermal studies suggested that the skin permeation of resveratrol was promoted by the effect of Chitosan hydrogel beads and increased resveratrol distribution in the skin. In vitro cytotoxicity showed that resveratrol-loaded NLC-Chitosan hydrogel beads did not exert a hazardous effect on L929 cells. Hence, NLC-Chitosan hydrogel beads might be a promising method for topical applications of resveratrol.

Preparation of Chitosan Nanoparticles for Protein Delivery by w/o/w Emulsion Solvent Evaporation and Simple Ionotropic Gelation Techniques

2007 ◽  
Vol 121-123 ◽  
pp. 751-754 ◽  
Author(s):  
Garnpimol C. Ritthidej ◽  
W. Pichayakorn ◽  
Chulalongkorn Kusonwiriyawong ◽  
V. Lipipun
Keyword(s):  
Protein Delivery ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Form Complex ◽  
Ionotropic Gelation

The purpose of this study was to prepare chitosan nanoparticles (CS NP) for controlled protein delivery. Two techniques, simple ionotropic gelation (method [I]) and w/o/w emulsion solvent evaporation containing ionotropic gelation (method [II]), were used to prepare CS NP. Tripolyphosphate (TPP) and Eudragit L100-55 (Eud) were used as anionic agents to form complex with cationic chitosan. Bovine serum albumin (BSA) was encapsulated into NP. The morphological characteristics, particle size and size distribution, protein entrapment efficiency, zeta potential, in vitro release, protein secondary structure and its integrity were investigated. The results showed that CS NP could be prepared by appropriate cationic and anionic ratios in both methods. Excess anionic agents resulted in particle aggregation of micron size. The median sizes of particles were between 0.127-0.273 mcm with method [I] provided the smallest size. The 0.02-0.10% BSA loaded preparations showed the same particle sizes and size distributions as blank preparations. SEM photomicrographs revealed that the obtained NP were spherical. Protein entrapment efficiency was between 47-84% and increased when decreasing the percentage of drug loading. The method [II] with TPP exhibited the highest protein entrapment efficiency, following by the method [II] with Eud and method [I] with TPP, respectively. The zeta potentials were positive. Prolonged in vitro protein release profiles were observed from all preparations of CS NP. After 10 days, the release was between 53-72%. Circular dichroism and SDS-polyaceylamide gel electrophoresis techniques confirmed that these processes did not have any destructive effect on the protein structure. Therefore these preparation techniques could be used to encapsulate water-soluble drugs, proteins, DNA, or antigens into CS NP as effective delivery carriers.

scholarly journals PARTIAL AMORPHIZATION OF POORLY-SOLUBLE SIMVASTATIN USP USING MEDIA MILLING IN SYNERGISM WITH SPRAY-DRYING

2020 ◽  
pp. 114-121
Author(s):  
HARITA R. DESAI ◽  
ARCHANA B. RAJADHYAX ◽  
PURNIMA D. AMIN
Keyword(s):  
Differential Scanning Calorimetry ◽  
Spray Drying ◽  
Scanning Calorimetry ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Media Milling ◽  
Rate Testing ◽  
Poorly Soluble ◽  
Spray Dried

Objective: The objective of the current study was to explore top down methods of size reduction like high speed homogenisation and media milling in synergism with spray drying in amorphization and solubility enhancement of BCS Class II antilipidemic drug Simvastatin USP. Methods: Spray-dried micronized simvastatin USP was formulated by homogenisation and media milling of drug suspension in optimized stabilizer solution. Stabilizer combination, duration of homogenisation and ball milling and drug: stabilizer ratio was optimized. The obtained dispersion was transformed into solid powder using spray drying. The obtained Spray-dried micronized Simvastatin USP was evaluated for visual morphology, Infrared spectroscopy, Differential scanning calorimetry, in vitro drug release studies, X-Ray diffractometry, Scanning electron microscopy, contact angle measurement, solubility studies, dispersibility studies and intrinsic dissolution rate testing. Results: Spray-dried micronized simvastatin USP was found to show amorphization of crystalline Simvastatin USP as confirmed by the absence of drug peak in Differential scanning calorimetry and lowered signal intensity in X-Ray diffraction studies. Spray-dried micronized Simvastatin USP was found to show enhanced drug hydrophilicity and solubility as confirmed by lowering in contact angle and increase in solubility and ease of dispersibility observations. In vitro dissolution testing and intrinsic dissolution rate testing were found to show an increase in drug release from 11% to 79% and 4 mg min-1 cm-2 to 17 mg min-1 cm-2 for drug and Spray-dried micronized Simvastatin USP respectively. Conclusion: Media milling in synergism with spray-drying was found to be a prospective solubility enhancement technique for poorly-soluble Simvastatin USP.

Comparison of Freeze and Spray Drying to Obtain Primaquine-Loaded Solid Lipid Nanoparticles

2021 ◽  
pp. 288-304
Author(s):  
James Jorum Owuor ◽  
Florence Oloo ◽  
Japheth Kibet Ngetich ◽  
Mwaiwa Kivunzya ◽  
Wesley Nyaigoti Omwoyo ◽  
...  
Keyword(s):  
Spray Drying ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Drug Release Profile ◽  
Solid Lipid ◽  
Freeze Dried ◽  
Spray Dried

This article describes how the spray drying and freeze drying of various nanosized Solid Lipid Nanoparticle (SLN) and the physicochemical attributes of the acquired particles were examined. Primaquine loaded Solid Lipid Nanoparticles dried by the two strategies is examined. Particles were characterised by determination of size, drug loading, encapsulation efficiency and surface morphology. In vitro and kinetic drug discharge models were also considered. Preparation parameters have no impact on the molecule morphology and properties, and the main parameter deciding the molecule attributes in the drug substance of the nanoparticle, either in the spraying or in the freezing technique of drying. The drug release profile of spray dried SLN is superior to that of the freeze dried SLN.

Preparation of ciprofloxacin-encapsulated poly-ε- caprolactone microcapsules by the solvent evaporation technique

e-Polymers ◽  
2013 ◽  
Vol 13 (1) ◽  
Author(s):  
Marta Przybyslawska ◽  
Aleksandra Amelian ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
Evaporation Technique

Abstract The objective of this study was to prepare ciprofloxacin (CIP) encapsulated poly-ε-caprolactone (PCL) microcapsules by the single emulsion oilin- water (o/w) solvent evaporation method. The obtained microcapsules were characterized for size, morphology, drug loading and entrapment efficiency. The physical state of microcapsules was determined by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). Storage stability, the in vitro drug release and mathematical modeling of drug release were also tested. It was found that obtained microcapsules had spherical shape and their size range was from 57.5 μm to 234.7 μm. The drug loading of microcapsules was from 1.72% to 11.02%. The optimal conditions of the encapsulation process include the drug/polymer ratio 2/1, using homogenizer for 5 min at 15000 rpm to disperse CIP in PCL solution and aqueous phase at pH 5.5. The results of CIP release study indicate that obtained microcapsules might be successfully used for designing sustained release dosage forms.

scholarly journals Poly (2-hydroxyethylmethacrylate –co–methylmethacrylate)/Lignocaine Contact Lens Preparation, Characterization, and in vitro Release Dynamic

Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 917 ◽  
Author(s):  
Taieb Aouak ◽  
Wassem Sharaf Saeed ◽  
Nawaf M. Al-Hafi ◽  
Abdel-Basit Al-Odayni ◽  
Abdulaziz Ali Alghamdi ◽  
...  
Keyword(s):  
Contact Lens ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Potential Candidate ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Drug Carrier System ◽  
Vitro Release ◽  
Carrier Systems

2-hydroxyethyl methacrylate, methylmethacrylate, ethylene glycol dimethyl methacrylate, and lignocaine (drug) were mixed together and the monomers were copolymerized at 60 °C through a free radical polymerization in the presence of α,α′-Azoisobutyronitrile in tetrahydrofuran. A series of copolymer/drug composites with different monoacrylate monomer compositions were prepared by solvent evaporation and characterized by different methods such as nuclear magnetic resonance, differential scanning calorimetry, Fourier transform infrared, X-ray diffraction, and mechanical and optical testing. The water content in the copolymers and the cell viability test on the samples were also examined in this investigation. The results of the analyses of the properties of this drug-carrier system are promising, indicating that this material may be a potential candidate for contact lens applications. The release dynamic of this medication from the prepared drug-carrier systems was investigated in neutral pH media. The results obtained revealed that the diffusion of lignocaine through the copolymer matrix obeys the Fick model and the dynamic release can be easily controlled by the methyl methacrylate content in the copolymer.

scholarly journals Celecoxib-loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics

2010 ◽  
Vol 30 (5) ◽  
pp. 365-373 ◽  
Author(s):  
Asli Deniz ◽  
Asli Sade ◽  
Feride Severcan ◽  
Dilek Keskin ◽  
Aysen Tezcaner ◽  
...  
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Cholesterol Content ◽  
High Plasma ◽  
Hydrophobic Core ◽  
Scanning Calorimetry ◽  
Liposome Size ◽  
Systemic Side Effects ◽  
Highly Hydrophobic

CLX (celecoxib) is a highly hydrophobic non-steroidal anti-inflammatory drug with high plasma protein binding. We describe here the encapsulation of CLX in MLVs (multilamellar vesicles) composed of DSPC (1,2-distearoyl-sn-glycero-3-phosphocholine) and variable amounts of cholesterol. The effects of cholesterol content on liposome size, percentage drug loading and in vitro drug release profiles were investigated. Differential scanning calorimetry and FTIR (Fourier-transform infrared) spectroscopy were used to determine molecular interactions between CLX, cholesterol and DSPC. The phase transition temperature (Tm) of vesicles was reduced in a synergistic manner in the presence of both CLX and cholesterol. Encapsulation efficiency, loading and release of CLX decreased with increasing cholesterol content. FTIR results indicated that this decrease was due to a competition between CLX and cholesterol for the co-operativity region of the phospholipids. In the presence of cholesterol, CLX was pushed further into the hydrophobic core of the bilayer. However, MLVs prepared with DSPC only (without cholesterol) exhibited the lowest ability for drug retention after 72 h. Our results indicated that CLX, without the requirement of modifications to enhance solubilization, can be encapsulated and released from liposomal formulations. This method of drug delivery may be used to circumvent the low bioavailability and systemic side effects of oral CLX formulations.

scholarly journals Development and Evaluation of Salbutamol Sulphate Loaded Ethyl Cellulose Microcapsules using Emulsion Solvent Evaporation Technique

2015 ◽  
Vol 18 (2) ◽  
pp. 132-136 ◽  
Author(s):  
Md Shamsul Alam ◽  
Jakir Ahmed Chowdhury ◽  
Sams Mohammad Anowar Sadat ◽  
Md Selim Reza
Keyword(s):  
Ethyl Cellulose ◽  
In Vitro Release ◽  
Solvent Evaporation ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Salbutamol Sulphate ◽  
Evaporation Technique ◽  
Vitro Release

Ethyl cellulose (EC) microcapsules containing Salbutamol sulphate (SS) were prepared through emulsion-solvent evaporation technique. Microcapsules were compressed and in-vitro release profiles were studied from both microcapsules and their compressed matrix tablets. Different amounts of drug were added in order to obtain various drugs to polymer ratios and it was found that the size of microcapsules reduced with the increase in core loading. In the preparation of formulations, Tween 80 was used as an emulsifying or dispersing agent and light liquid paraffin (LLP) was used as oil phase. The in-vitro release of EC microcapsules was studied in distilled water at 37º ± 0.5°C. A biphasic release behavior of SS from microcapsules was observed. In case of microcapsules, an immediate release was observed but for their compressed tablet form, initially a burst effect and then slow release were observed which was extended for 8 hours. In order to further investigate the type of drug release mechanism, the dissolution data were plotted according to the different kinetic models. In-vitro dissolution studies showed that zero-order and square-root of time (Higuchi model) release characteristics were exhibited.Bangladesh Pharmaceutical Journal 18(2): 132-136, 2015

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