scholarly journals Influence of Solvent Evaporation Technique Parameters on Diameter of Submicron Lamivudine-Poly-ε-Caprolactone Conjugate Particles

Nanomaterials ◽  
2019 ◽  
Vol 9 (9) ◽  
pp. 1240 ◽  
Author(s):  
Tomasz Urbaniak ◽  
Witold Musiał
Keyword(s):  
Drug Loading ◽  
Particle Diameter ◽  
Active Pharmaceutical Ingredient ◽  
Solvent Evaporation ◽  
Poly Vinyl Alcohol ◽  
Polymeric Chain ◽  
Polymer Conjugate ◽  
Homogenization Rate ◽  
Evaporation Technique ◽  
Particle Preparation

The size of active pharmaceutical ingredient carrier is one of the key properties considered during design of submicron drug delivery systems. Particle diameter may determine drug biodistribution, cellular uptake, and elimination path. Solvent evaporation technique is a flexible method of particle preparation, in which various macromolecules and drugs may be employed. Parameters of emulsion obtained as first step of particle preparation are crucial in terms of particle size, drug loading, and morphology. The aim of the study was to investigate the influence of emulsion preparation parameters on diameter of resulting particles. Impact of surfactant type and concentration, homogenization time, homogenization rate, phase ratio, and conjugate concentration were evaluated. Model drug lamivudine was covalently bound to polymer and applied in solvent evaporation method in order to overcome issues related to drug loading and provide method-independent incorporation. Synthesized drug–polymer conjugate and obtained particles were evaluated via dynamic light scattering, chromatography, scanning electron microscopy, and spectroscopic methods. Covalent bonding between drug and polymeric chain was confirmed, estimated drug content per milligram of conjugate was 19 μg. Among employed colloid stabilizer, poly(vinyl alcohol) was proven to be most effective. Homogenization rate and surfactant concentration were identified as crucial parameters in terms of particle diameter control.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

scholarly journals Solubility Enhancement of Diclofenac Using Solid Dispersions

2021 ◽  
Vol 5 (1) ◽  
pp. 1-6
Author(s):  
Mohd. Aamir Mirza ◽  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Diclofenac Sodium ◽  
Active Pharmaceutical Ingredient ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Limiting Factor ◽  
Formulation Development ◽  
Enhanced Solubility ◽  
Evaporation Technique

Background: The phenomenon which gives rise to a homogenous system, formed by the dissolution of solute in a solvent is known as solubility. Low solubility is the limiting factor in formulation development. Diclofenac being BCS class II drug have low aqueous solubility of 0.00401mg/ml. Amongst various solubility enhancement techniques, solid dispersion is the easiest one. Objective: Present work is primarily focused on the development of solid dispersions of diclofenac through solvent evaporation technique utilizing Eudragit E100 as a carrier. Methods: Solid dispersion consists of at least one active pharmaceutical ingredient as a carrier in solid state. Various methods for preparing solid dispersions includes melt extrusion, fusion lyophilization, spray drying, solvent evaporation, and super critical fluid (SCF) technology. Solvent evaporation technique is used among various solid dispersion methods. Conclusion: The enhanced solubility found to be 0.485mg/ml. The dissolution was performed using USP Type II apparatus was %CDR of pure drug and its solid dispersion in 8 hr were found out to be 45.14926% and 98.04758% respectively. Henceforth, solid dispersion technique results marked solubility enhancement of diclofenac sodium.

scholarly journals Encapsulation of metronidazole in polycaprolactone microspheres

2019 ◽  
Vol 9 (1) ◽  
pp. 190-194
Author(s):  
Rima Kassab ◽  
Dima Moussa ◽  
Cherine Saliba ◽  
Paolo Yammine
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
Compatibility Study ◽  
Drug Encapsulation ◽  
Evaporation Technique ◽  
Ft Ir ◽  
Ir Study

Non-aqueous oil-in-oil solvent evaporation technique is used for the preparation of polycaprolactone microspheres loaded with the antibiotic metronidazole by introducing different masses for the drug. The prepared microspheres are characterized by calculating drug encapsulation and drug loading percentages, measuring the corresponding particle size, performing FT-IR polymer-drug compatibility study and in vitro drug release. Moderate drug encapsulation values with a maximum of 34% are observed due to the low molecular weight of the drug. Microspheres had a particle size ranging between 130 and 280 µm with a spherical profile and porous structure. FT-IR study showed no interactions between the drug and the polymer. Drug release studies showed fast release rates for all the formulations with the slowest release for the highest drug loading. Keywords: polycaprolactone, metronidazole, targeted drug delivery, solvent evaporation.

scholarly journals Preparation and Characterization of Polyvinyl Acetate (Kollidon® SR) Microspheres Containing Diclofenac Sodium II: Effect of core loading

1970 ◽  
Vol 8 (2) ◽  
pp. 117-122
Author(s):  
Md Saiful Islam ◽  
Ashfacur Rahman ◽  
Mohammad Kaisarul Ismal ◽  
Jakir Ahmed Chowdhury ◽  
Reza-ul Jalil
Keyword(s):  
Encapsulation Efficiency ◽  
Polyvinyl Acetate ◽  
Drug Loading ◽  
Diclofenac Sodium ◽  
Solvent Evaporation ◽  
Dissolution Time ◽  
Release Rates ◽  
Mean Dissolution Time ◽  
Evaporation Technique ◽  
Microsphere Size

Diclofenac Sodium (DS) loaded Kollidon® SR (Polyvinyl acetate and povidone based matrix retarding polymer) microspheres of different drug loading were prepared using W/O emulsification solvent evaporation technique. Polymeric solution containing the DS was emulsified in light liquid paraffin (LLP) which was initially emulsified by 1% (w/w of the continuum) lipophilic surfactant Span 60. The study was conducted to investigate the effect of different core to polymer ratio (0.5: 1, 1 : 1, 1.5 : 1 and 2 : 1) on microsphere size, encapsulation efficiency and release kinetics of DS. Microsphere size was decreased with increased core loading. However, higher encapsulation efficiency was observed with higher core loading. A square root of time dependent release of DS was observed from the KSR microspheres. Increased core loading caused faster release of DS. Release rates of DS were affected by different DS content in the core. Normalized release rates were also found to be increased with high core loading. Mean dissolution time (MDT) and t50 values were also calculated and were found to be affected significantly by different DS loading to KSR microspheres. Low DS loading increased MDT. Key words: Kollidon® SR; Diclofenac Sodium; Microsphere; Solvent evaporation technique; Mean dissolution time. DOI: 10.3329/dujps.v8i2.6025 Dhaka Univ. J. Pharm. Sci. 8(2): 117-122, 2009 (December)

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 Effect of Cellulosic and Polymethacrylic Polymers on Drug Content, Particle Morphology, and Carbamazepine Release Profiles from Sustained Release Ethyl Cellulose Microspheres

1970 ◽  
Vol 9 (2) ◽  
pp. 75-82 ◽  
Author(s):  
Sams Mohammad Anowar Sadat ◽  
Md Saiful Islam ◽  
Sheikh Tasnim Jahan ◽  
Jakir Ahmed Chowdhury ◽  
Reza-ul Jalil
Keyword(s):  
Sustained Release ◽  
Release Rate ◽  
Ethyl Cellulose ◽  
Sodium Dodecyl ◽  
In Vitro Release ◽  
Particle Diameter ◽  
Solvent Evaporation ◽  
Drug Content ◽  
Key Words Carbamazepine ◽  
Evaporation Technique

Emulsion-solvent evaporation technique was used to prepare Carbamazepine (CBZ) loaded Ethyl Cellulose (EC) microspheres. Cellulosic polymers (HPMC 4.5 cps, 15 cps) and polymethacrylic polymers (Eudragit E100, Eudragit RL PO, Eudragit RS PO) were added with EC at 10% (w/w) of EC. The effect of these polymers on drug content, particle size, and CBZ release rate were evaluated. The CBZ encapsulation efficiency and the drug content varied from 85% to 95% and from 42% to 45% (w/w), respectively. The mean particle diameter varied from 460 to 730 μm. In vitro release study for 8 hours was conducted in 1% (w/v) sodium dodecyl sulfate solution. All the polymers reduced the release of CBZ and a statistically significant variation in release rate was observed from polymer to polymer. Key words: Carbamazepine; Ethyl Cellulose; Sustained release microspheres; Emulsion-Solvent Evaporation Technique. DOI: http://dx.doi.org/10.3329/dujps.v9i2.7883 Dhaka Univ. J. Pharm. Sci. 9(2): 75-82, 2010 (December)  

scholarly journals Preparation and Characterization of Polyvinyl Acetate (Kollidon® SR) Microspheres Containing Diclofenac Sodium I: Effect of Stirring Rate and Total Solid Content

1970 ◽  
Vol 8 (2) ◽  
pp. 111-116 ◽  
Author(s):  
Md Saiful Islam ◽  
Sayed Md Reazul Alam ◽  
Sams Mohammad Anowar Sadat ◽  
Jakir Ahmed Chowdhury ◽  
Reza-ul Jalil
Keyword(s):  
Drug Loading ◽  
Diclofenac Sodium ◽  
Total Solid ◽  
Solvent Evaporation ◽  
Solid Content ◽  
In Vitro Dissolution ◽  
Total Solid Content ◽  
Stirring Rate ◽  
Evaporation Technique ◽  
The Continuum

Microspheres were prepared by W/O emulsification solvent evaporation technique where Diclofenac Sodium (DS) and Kollidon® SR (KSR) were used as model drug and polymer respectively. Light liquid paraffin (LLP) was used as oil phase and 1% (w/w of the continuum) of span 60 was used for emulsification. Microspheres were prepared using different stirring rate (1500, 2000, 2500, 3000 rpm) and different total solid content of the system (0.08%, 0.16%, 0.24% w/w of the continuum). Microsphere morphology was examined with the help of Scanning Electron Microscope (SEM) and particle size distribution was analyzed by Mastersizer 2000. Larger microspheres were obtained with decreasing stirring rate. Increase in solid content of the system also increased microsphere size. Drug loading was also found to be affected due to these preparative variables. In vitro dissolution study was performed in a USP XXX paddle apparatus (type 2). Dissolution media was buffer of pH 7.2, paddle speed was 50 rpm and dissolution temperature was maintained at 37 ± 0.5°C. Release of DS from KSR microspheres was found to follow higuchi mechanism. DS release was increased with increased stirring rate. But increased solid content of the system resulted in reduced release of DS. Normalized release rate of DS was also found to be affected by these preparative variables. Release rates were found increased with increased stirring rate whereas rates were found decreased with increased solid content of the system. Key words: Kollidon® SR; Diclofenac Sodium; Microsphere; Solvent evaporation technique. 10.3329/dujps.v8i2.6024 Dhaka Univ. J. Pharm. Sci. 8(2): 111-116, 2009 (December)

scholarly journals Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of Phoenix dactylifera L. of 5-Fluorouracil for Colon-Specific Drug Delivery

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1921
Author(s):  
Mohammad Raish ◽  
Mohd Abul Kalam ◽  
Ajaz Ahmad ◽  
Mudassar Shahid ◽  
Mushtaq Ahmad Ansari ◽  
...  
Keyword(s):  
Gastrointestinal Tract ◽  
Targeted Delivery ◽  
Direct Method ◽  
Drug Loading ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Phoenix Dactylifera ◽  
Solvent Evaporation ◽  
Maximum Plasma ◽  
Evaporation Technique

In this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux method and 5-FU into SEMC was encapsulated by the vacuum-assisted loading method. 5-FU loaded SEMC was coated with Eudragit® RS-100 (ERS) by the organic solvent-evaporation technique under vacuum to avoid the discharge of 5-FU in the stomach and small intestine. Morphological and physicochemical characterization of drug-loaded SEMC (coated/uncoated) was performed by scanning electron microscopy (SEM), FTIR, XRD, and DSC. The encapsulation and drug loading were determined by the direct method, and an in vitro release study was performed in simulated gastric and intestinal fluids (SGF/SIF). The colon-specific delivery of 5-FU from the SEMC was assessed in terms of pharmacokinetics and gastrointestinal tract distribution after oral administration in rats. The successful encapsulation and loading of 5-FU into SEMC by a vacuum-assisted loading technique and its coating with ERS by a solvent-evaporation technique were achieved. SEM images of uncoated SEMC have shown porous structures, and coating with ERS reserved their morphology with a smooth surface and discrete microstructures and the 5% w/v ERS acetone solution. ERS-coated SEMC sustained the release of 5-FU until 24 h in SIF, while it was up to 12 h only from uncoated SEMC. The maximum plasma concentration (Cmax) of 5-FU from uncoated SEMC was 102.82 μg/mL after 1 h, indicating a rapid release of 5-FU in the upper gastrointestinal tract. This concentration decreased quickly with a half-life of 4 h, AUC0-t was 264.1 μg/mL.h, and MRT0-inf was 5.2 h. The Cmax of 5-FU from ERS-coated SEMC was 19.47 μg/mL at 16 h. The Cmax of 5-FU in small intestines was 406.2 μg/g at 1 h from uncoated SEMC and 1271.5 μg/g at 12 h from coated SEMC. Conclusively, a 249.9-fold higher relative bioavailability of 5-FU was achieved with the ERS-coated SEMC in colon tissues than that from uncoated SEMC.

The Effect of Phase Transition Temperature on Therapeutic Efficacy of Liposomal Bortezomib

2020 ◽  
Vol 20 (6) ◽  
pp. 700-708
Author(s):  
Mitra Korani ◽  
Sara Nikoofal-Sahlabadi ◽  
Amin R. Nikpoor ◽  
Solmaz Ghaffari ◽  
Hossein Attar ◽  
...  
Keyword(s):  
Side Effects ◽  
Cell Line ◽  
Therapeutic Efficacy ◽  
Drug Loading ◽  
Particle Diameter ◽  
In Vitro Cytotoxicity ◽  
Liposomal Formulations ◽  
Cytotoxicity Studies ◽  
Anti Tumor Activity

Aims: Here, three liposomal formulations of DPPC/DPPG/Chol/DSPE-mPEG2000 (F1), DPPC/DPPG/Chol (F2) and HSPC/DPPG/Chol/DSPE-mPEG2000 (F3) encapsulating BTZ were prepared and characterized in terms of their size, surface charge, drug loading, and release profile. Mannitol was used as a trapping agent to entrap the BTZ inside the liposomal core. The cytotoxicity and anti-tumor activity of formulations were investigated in vitro and in vivo in mice bearing tumor. Background: Bortezomib (BTZ) is an FDA approved proteasome inhibitor for the treatment of mantle cell lymphoma and multiple myeloma. The low solubility of BTZ has been responsible for the several side effects and low therapeutic efficacy of the drug. Encapsulating BTZ in a nano drug delivery system; helps overcome such issues. Among NDDSs, liposomes are promising diagnostic and therapeutic delivery vehicles in cancer treatment. Objective: Evaluating anti-tumor activity of bortezomib liposomal formulations. Methods: Data prompted us to design and develop three different liposomal formulations of BTZ based on Tm parameter, which determines liposomal stiffness. DPPC (Tm 41°C) and HSPC (Tm 55°C) lipids were chosen as variables associated with liposome rigidity. In vitro cytotoxicity assay was then carried out for the three designed liposomal formulations on C26 and B16F0, which are the colon and melanoma cancer mouse-cell lines, respectively. NIH 3T3 mouse embryonic fibroblast cell line was also used as a normal cell line. The therapeutic efficacy of these formulations was further assessed in mice tumor models. Result: MBTZ were successfully encapsulated into all the three liposomal formulations with a high entrapment efficacy of 60, 64, and 84% for F1, F2, and F3, respectively. The findings showed that liposomes mean particle diameter ranged from 103.4 to 146.8nm. In vitro cytotoxicity studies showed that liposomal-BTZ formulations had higher IC50 value in comparison to free BTZ. F2-liposomes with DPPC, having lower Tm of 41°C, showed much higher anti-tumor efficacy in mice models of C26 and B16F0 tumors compared to F3-HSPC liposomes with a Tm of 55°C. F2 formulation also enhanced mice survival compared with untreated groups, either in BALB/c or in C57BL/6 mice. Conclusion: Our findings indicated that F2-DPPC-liposomal formulations prepared with Tm close to body temperature seem to be effective in reducing the side effects and increasing the therapeutic efficacy of BTZ and merits further investigation.

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