Evaluation of oral carvedilol microparticles prepared by simple emulsion technique using poly(3-hydroxybutyrate-co-3-hydroxyvalerate) and polycaprolactone as polymers

Riekes, Manoela Klüppel; Barboza, Fernanda Malaquias; Vecchia, Débora Dalla; Bohatch, Milton Sérgio; Farago, Paulo Vítor; Fernandes, Daniel; Silva, Marcos Antônio Segatto; Stulzer, Hellen Karine

doi:10.1016/j.msec.2011.02.017

Cited by 26 publications

(13 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…These results indicate that PCL formulations are more thermally stable than PHBV formulations. Similar results have been described in the literature for PCL and PHBV microparticles [ 24 , 27 ].…”

Section: Resultssupporting

confidence: 90%

See 1 more Smart Citation

PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride

Barboza

Machado

Olchanheski

et al. 2014

The Scientific World Journal

Self Cite

View full text Add to dashboard Cite

Microparticles of poly(ε-caprolactone) (PCL) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing manidipine dihydrochloride (MAN) were successfully prepared by the simple emulsion/solvent evaporation method. All formulations showed loading efficiency rates greater than 80% and average particle size less than 8 μm. Formulations had spherical shape with smooth and porous surface for PCL and PHBV, respectively. According to Fourier-transform infrared spectroscopy, initial components were not chemically modified during microencapsulation. X-ray diffraction patterns and differential scanning calorimetry demonstrated that this process led to drug amorphization. In vitro dissolution studies showed that all microparticles prolonged MAN release, mainly which one obtained using PCL that contained 5% of drug loaded (PCL-M5). Animal studies demonstrated that formulation PCL-M5 was able to keep the variation of mean arterial pressure after phenylephrine administration up to 24 hours. These data confirmed the sustained antihypertensive effect of the investigated microparticles. Results provided an experimental basis for using formulation PCL-M5 as a feasible carrier for oral controlled release of MAN intended for treating high blood pressure.

show abstract

Section: Resultssupporting

confidence: 90%

“…In general, amorphous solids dissolve more quickly than crystalline forms, due to free energies involved in their dissolution process. Solids in amorphous state have randomly arranged molecules; thus, low energy is required to separate them what makes their dissolution faster when compared to crystalline form [ 24 ].…”

Section: Resultsmentioning

confidence: 99%

PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride

Barboza

Machado

Olchanheski

et al. 2014

The Scientific World Journal

Self Cite

View full text Add to dashboard Cite

show abstract

“…The polyester microparticles containing FA were prepared by simple emulsion/solvent evaporation [ 22 ]. Three different formulations ( Table 2 ) were obtained for each polymer (PHBV/PCL) depending on the amount of FA into their compositions (5, 10, and 20%).…”

Section: Methodsmentioning

confidence: 99%

A Stability-Indicating HPLC-DAD Method for Determination of Ferulic Acid into Microparticles: Development, Validation, Forced Degradation, and Encapsulation Efficiency

Nadal

Toledo

Pupo

et al. 2015

Journal of Analytical Methods in Chemistry

Self Cite

View full text Add to dashboard Cite

A simple stability-indicating HPLC-DAD method was validated for the determination of ferulic acid (FA) in polymeric microparticles. Chromatographic conditions consisted of a RP C18 column (250 mm × 4.60 mm, 5 μm, 110 Å) using a mixture of methanol and water pH 3.0 (48 : 52 v/v) as mobile phase at a flow rate of 1.0 mL/min with UV detection at 320 nm. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of quantification, limit of detection, accuracy, precision, and robustness provided suitable results regarding all parameters investigated. The calibration curve was linear in the concentration range of 10.0–70.0 μg/mL with a correlation coefficient >0.999. Precision (intraday and interday) was demonstrated by a relative standard deviation lower than 2.0%. Accuracy was assessed by the recovery test of FA from polymeric microparticles (99.02% to 100.73%). Specificity showed no interference from the components of polymeric microparticles or from the degradation products derived from acidic, basic, and photolytic conditions. In conclusion, the method is suitable to be applied to assay FA as bulk drug and into polymeric microparticles and can be used for studying its stability and degradation kinetics.

show abstract

“…These peaks were not observed in the CRV loaded gastrospheres. This indicates that drug particles are dispersed at molecular level in the polymer matrices since no indication about the crystalline nature of the drugs was observed in the drug-loaded gastrospheres [23][24][25][26].…”

Section: Xrd Analysismentioning

confidence: 99%

“…The SEM photographs indicated that the gastrospheres were completely covered with polymer the rough texture which may be due to removal of water from gastrospheres during drying. Thus the rate of removal of water from gastrospheres exerts an influence on the morphology of final product [23][24][25][26][27][28].…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Design, Development, and Characterization of Ocimum Basilicum Mucilage-Based, Modified Release Mucoadhesive Gastrospheres of Carvedilol

FJ²

2019

Asian J Pharm Clin Res

View full text Add to dashboard Cite

Objective: The present investigations aim to develop mucoadhesive gastrospheres of carvedilol using sodium alginate and Ocimum basilicum seed mucilage combination blend oral use. Methods: The gastrospheres were prepared by ionotropic gelation method using 32 factorial designs, the concentration of sodium alginate and O. basilicum mucilage was independent variables while % drug content (DC), % entrapment efficiency, and % drug release at 12 h were dependent variables. The gastrospheres were evaluated for other parameters such as Fourier-transform infrared (FTIR), powder X-ray diffraction, differential scanning calorimetric, and in vitro mucoadhesion studies. Results: In optimization studies from statistical second-order complete model equation among the polymers used O. basilicum mucilage had a more profound effect on DC and % encapsulation efficiency as compared to sodium alginate. The mean particle size of gastrospheres when measured by optical microscopy technique ranged from 774 to 882 μm. The percentage of gastrosphere adhering to goat intestinal mucosal tissue varied from 10% to 65% over 8 h in 0.1N HCl, whereas this was varied from 40% to 60% in phosphate buffer pH 6.8 with provided 12 h of controlled release following zero-order release pattern. Conclusion: Studies conclude that mucilage of O. basilicum can be used as controlled release mucoadhesive material in the formulation of gastrospheres.

show abstract

Evaluation of oral carvedilol microparticles prepared by simple emulsion technique using poly(3-hydroxybutyrate-co-3-hydroxyvalerate) and polycaprolactone as polymers

Cited by 26 publications

References 21 publications

PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride

PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride

A Stability-Indicating HPLC-DAD Method for Determination of Ferulic Acid into Microparticles: Development, Validation, Forced Degradation, and Encapsulation Efficiency

Design, Development, and Characterization of Ocimum Basilicum Mucilage-Based, Modified Release Mucoadhesive Gastrospheres of Carvedilol

Contact Info

Product

Resources

About