Preparation of amphiphilic cyclodextrin nanospheres using the emulsification solvent evaporation method. Influence of the surfactant on preparation and hydrophobic drug loading

1998 ◽  
Vol 170 (1) ◽  
pp. 119-128 ◽  
Author(s):  
E. Lemos-Senna ◽  
D. Wouessidjewe ◽  
S. Lesieur ◽  
D. Duchêne
1970 ◽  
Vol 7 (5) ◽  
pp. 30-36
Author(s):  
Sandeep A Wathore

The formulation of floating microspheres of Betahistine hydrochloride by the o/w emulsification and solvent evaporation method in the presence of tween 80 as an emulsifying agent. The influence of formulation factor Drug: Polymer ratio on particle size, encapsulation efficiency and invitro release characteristics of the microspheres were investigated. The microspheres have been analyzed for their size, drug loading capacity and drug release study. Spherical and smooth surfaced microspheres with desired encapsulation efficiencies were obtained. Slow drug release from microspheres observed up to 12 h. for formulation F4, F5. Optimized formulation F4 was evaluated for FTIR, DSC, SEM. DSC and FTIR studies showed that the nature of pure drug Betahistine hydrochloride remains unaffected till the completion of process of microspheres formation. SEM photographs showed that the Floating microspheres were spherical in nature with smooth surface and uniform distribution of the drug within the microsphere. Keywords: 


2011 ◽  
Vol 695 ◽  
pp. 517-520
Author(s):  
Pei Pei Luo ◽  
Ji Dong Li ◽  
Yi Zuo ◽  
Xia Wu ◽  
Yu Bao Li

In this paper, isoniazid (INH)-loaded poly (ε-caprolactone) microspheres with a special microporous surface and relatively high drug loading were fabricated by an oil-in-oil (O/O) solvent evaporation method. Meanwhile the microspheres were produced by an oil-in-water (O/W) method for comparison. The technological parameters such as the concentration of surfactant, the volume of continuous phase and the quantity of the drug were investigated systematically. The microspheres morphology, their size distribution and the viscosity of both the dispersed and continuous phase were characterized. The results indicate that the O/O solvent evaporation method is a feasible approach to encapsulate micromolecular and hydrophilic drugs in PCL. This opens the door for INH-loaded microspheres able to release drugs and thereby improve the therapy of tuberculosis of bones and joints in the future.


2013 ◽  
Vol 16 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Nandini Saha ◽  
Ikramul Hasan ◽  
Mehrina Nazmi ◽  
Md Selim Reza

Ibuprofen, a non-steroidal anti-inflammatory drug was formulated as microspheres by using Methocel K4M & Eudragit RSPO. These microspheres were prepared by emulsification solvent evaporation method to provide sustained action and to minimize local side effect of Ibuprofen by avoiding the drug release in the upper gastrointestinal tract. The prepared microspheres were subjected to various evaluation and in-vitro release studies. In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) using Phosphate buffer (pH 7.4) as the dissolution medium at 37.5oC for 6 hours (paddle speed 50 RPM). The release mechanisms were explored and explained with Zero Order, First Order, Higuchi and Korsmeyer-Peppas equations. The correlation coefficients values of the trend lines of the graphs showed that the formulations best fit with Korsmeyer-Peppas release pattern. Microspheres’ morphology and chemical integrity were studied by a scanning electron microscope (SEM) and Fourier transforms infrared spectroscopy (FTIR) respectively. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14489 Bangladesh Pharmaceutical Journal 16(1): 39-44, 2013


2021 ◽  
Vol 18 (4) ◽  
pp. 733-741 ◽  
Author(s):  
Paroma Arefin ◽  
Md Shehan Habib ◽  
Mohammad Mostafa ◽  
Dipankar Chakraborty ◽  
Sreebash Chandra Bhattacharjee ◽  
...  

Microspheres, a potential drug delivery approach, has opened a new era for attaining versatile release patterns needed. By optimizing the formulation variables, they can be prepared to obtain targeted release, immediate release, sustained release patterns. The release of the active drug material depends upon a number of formulation parameters such as polymers, stirring speed (rpm), methodology, surfactants, etc. Fexofenadine hydrochloride (HCl) is a second generation antihistamine. Our present research has explored the effects of using different rpm (600- 1000 rpm) in preparing fexofenadine hydrochloride (HCl) microspheres by emulsion solvent evaporation method. The formulation is aimed to provide sustained release for the required long period with a high margin of safety. We used a blended mixture of Hydroxy Propyl Methyl Cellulose (HPMC) K 100 MCR and Eudragit RL100 polymers to have sustained-release microspheres. The impact of different rpm on Yield, drug encapsulation efficiency, flow properties, and dissolution pattern were appraised. We observed the release of the drug for 10 hours in phosphate buffer (pH 6.8) and evaluated the drug release spectrophotometrically. Our study finds that the release of fexofenadine HCl from the microspheres was significantly increased with drug loading. We found the dosage forms to follow Higuchi release kinetics and Hixson-Crowell release kinetics the most, indicating successful achievement of sustained-release pattern in the dosage form. The change in drug release rate was statistically significant for variation in the stirring rate. We found that 600 rpm was the most optimized stirring rate for preparing microspheres in the emulsion solvent evaporation method.


Author(s):  
Ninda Sukmaningrum ◽  
Lusia Oktora Ruma Kumala Sari ◽  
Eka Deddy Irawan

Metformin hidroklorida (MH) merupakan obat pilihan pertama yang digunakan dalam terapi diabetes mellitus tipe 2, namun dapat menimbulkan efek samping pada saluran pencernaan sehingga MH tepat dipreparasi menjadi sediaan microspheres. Banyak faktor yang mempengaruhi hasil preparasi microspheres di antaranya adalah konsentrasi etil selulosa (EC) dan lama pengadukan yang digunakan. Penelitian ini bertujuan untuk mengetahui komposisi terbaik konsentrasi EC dan lama pengadukan yang dapat menghasilkan microspheres MH-EC dengan entrapment efficiency (EE) tertinggi menggunakan optimasi desain faktorial. MH digunakan sebagai bahan aktif, EC digunakan sebagai polimer serta non-aqueous solvent evaporation method sebagai teknik yang dipilih dalam preparasi microspheres. Hasilnya microspheres yang menggunakan konsentrasi EC sebanyak 4.500 mg dan lama pengadukan selama 2 jam menghasilkan EE sebesar 84,6 ± 0,557% dengan nilai verifikasi EE sebesar 98,1%, drug loading sebesar 12,7 ± 0,173% dan yield sebesar 95,1 ± 0,612%. Microspheres memiliki bentuk sferis dan morfologi permukaan yang relatif halus dan cerah serta ukuran partikel sebesar 173,8 ± 4,41µm. Hasil analisis FTIR menunjukkan bahwa tidak ada perubahan gugus fungsi spesifik pada MH sebagai bahan aktif. Kata kunci:    microspheres, metformin hidroklorida, etil selulosa


e-Polymers ◽  
2010 ◽  
Vol 10 (1) ◽  
Author(s):  
Jun Cao ◽  
Yuanwei Chen ◽  
Niancao Chen ◽  
Xianglin Luo

AbstractPhosphorylcholine-containing poly(L-lactide) (PLLA-PC) is a kind of amphiphilic copolymer synthesized with L-lactide (LLA) as monomer and glycerophosphorylcholine as ring-opening reagent. In this paper, self-assembly nanoparticles of PLLA-PC were prepared with solvent evaporation method. The factors that affected the properties and stability of nanoparticles were investigated. Transmission electron microscope (TEM) indicated that PLLA-PC nanoparticles presented typical core/shell structure. The critical micelle concentration (CMC) was determined with fluorescent probe method. The results showed that the CMCs were quite low (< 1×10-3 g/l) and were dependent on LLA units in the copolymer. The size of the nanoparticles was detected by dynamic light scattering (DLS). The results indicated that the size could be affected by LLA units, the amount of solvent and water in the preparation process. On the other hand, the obtained nanoparticles were stable while being stored at 4 °C, and hardly changed over the dilution with water, which was of great importance in venous injection. The solubility of clofazimine was better in aqueous solution of PLLA-PC nanoparticles than in pure water. This preliminary study suggested that PLLA-PC nanoparticles had a great potential as delivery system for hydrophobic drug.


Author(s):  
Taha A. Basher ◽  
Entidhar J. Muhammad

Itraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients. The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles. Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of   ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula  with composition of  ITZ(200mg), a first coat of HPMC15cps (200mg), a second coat of EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) which prepared by a dual coating solvent evaporation method using a first coat which provides relatively pH-independent solubility, while the second coat applied as a bouncy producing agents. Polyvinyl alcohol (PVA) was used as a surfactant in both cases. The prepared floating microparticles were subjected to various evaluation parameters such as yield percent, drug loading and drug entrapment efficiency (EE), particle size analysis, in- vitro bouncy, drug release, Fourier Transforms Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffractometry (XRD) studies.


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