Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation
Rai Muhammad Sarfraz,1 Mahmood Ahmad,2 Asif Mahmood,3 Muhammad Rouf Akram,1 Asad Abrar2 1Faculty of Pharmacy, University of Sargodha, Sargodha, 2Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur, 3Institute of Pharmacy, Physiology and Pharmacology, Univ...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Dove Medical Press
2017-10-01
|
| Series: | Drug Design, Development and Therapy |
| Subjects: | |
| Online Access: | https://www.dovepress.com/development-of-beta-cyclodextrin-based-hydrogel-microparticles-for-sol-peer-reviewed-article-DDDT |
| _version_ | 1818909431885201408 |
|---|---|
| author | Sarfraz RM Ahmad M Mahmood A Akram MR Abrar A |
| author_facet | Sarfraz RM Ahmad M Mahmood A Akram MR Abrar A |
| author_sort | Sarfraz RM |
| collection | DOAJ |
| description | Rai Muhammad Sarfraz,1 Mahmood Ahmad,2 Asif Mahmood,3 Muhammad Rouf Akram,1 Asad Abrar2 1Faculty of Pharmacy, University of Sargodha, Sargodha, 2Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur, 3Institute of Pharmacy, Physiology and Pharmacology, University of Agriculture Faisalabad, Faisalabad, Pakistan Abstract: The aim of this study was to enhance the solubility of rosuvastatin (RST) calcium by developing β-cyclodextrin-g-poly(2-acrylamido-2-methylpropane sulfonic acid [AMPS]) hydrogel microparticles through aqueous free-radical polymerization technique. Prepared hydrogel microparticles were characterized for percent entrapment efficiency, solubility studies, Fourier transform infrared spectroscopy, differential scanning calorimetry, thermal gravimetric analysis, powder X-ray diffraction, scanning electron microscopy, zeta size and potential, swelling and release studies. Formulations (HS1–HS9) have shown entrapment efficiency between 83.50%±0.30% and 88.50%±0.25%, and optimum release was offered by formulation HS7 at both pH levels, ie, 1.2 (89%) and 7.4 (92%). The majority of microparticles had a particle size of less than 500 µm and zeta potential of –37 mV. Similarly, optimum solubility, ie, 10.66-fold, was determined at pH 6.8 as compared to pure RST calcium, ie, 7.30-fold. In vivo studies on fabricated hydrogel microparticulate system in comparison to pure drug were carried out, and better results regarding pharmacokinetic parameters were seen in the case of hydrogel microparticles. A potential approach for solubility enhancement of RST calcium and other hydrophobic moieties was successfully developed. Keywords: hydrogel microparticles, rosuvastatin calcium, polymerization, β-cyclodextrin solubility |
| first_indexed | 2024-12-19T22:26:49Z |
| format | Article |
| id | doaj.art-eb6372c821254152aaa7ce0cb02510d6 |
| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-12-19T22:26:49Z |
| publishDate | 2017-10-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Drug Design, Development and Therapy |
| spelling | doaj.art-eb6372c821254152aaa7ce0cb02510d62022-12-21T20:03:30ZengDove Medical PressDrug Design, Development and Therapy1177-88812017-10-01Volume 113083309635292Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluationSarfraz RMAhmad MMahmood AAkram MRAbrar ARai Muhammad Sarfraz,1 Mahmood Ahmad,2 Asif Mahmood,3 Muhammad Rouf Akram,1 Asad Abrar2 1Faculty of Pharmacy, University of Sargodha, Sargodha, 2Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur, 3Institute of Pharmacy, Physiology and Pharmacology, University of Agriculture Faisalabad, Faisalabad, Pakistan Abstract: The aim of this study was to enhance the solubility of rosuvastatin (RST) calcium by developing β-cyclodextrin-g-poly(2-acrylamido-2-methylpropane sulfonic acid [AMPS]) hydrogel microparticles through aqueous free-radical polymerization technique. Prepared hydrogel microparticles were characterized for percent entrapment efficiency, solubility studies, Fourier transform infrared spectroscopy, differential scanning calorimetry, thermal gravimetric analysis, powder X-ray diffraction, scanning electron microscopy, zeta size and potential, swelling and release studies. Formulations (HS1–HS9) have shown entrapment efficiency between 83.50%±0.30% and 88.50%±0.25%, and optimum release was offered by formulation HS7 at both pH levels, ie, 1.2 (89%) and 7.4 (92%). The majority of microparticles had a particle size of less than 500 µm and zeta potential of –37 mV. Similarly, optimum solubility, ie, 10.66-fold, was determined at pH 6.8 as compared to pure RST calcium, ie, 7.30-fold. In vivo studies on fabricated hydrogel microparticulate system in comparison to pure drug were carried out, and better results regarding pharmacokinetic parameters were seen in the case of hydrogel microparticles. A potential approach for solubility enhancement of RST calcium and other hydrophobic moieties was successfully developed. Keywords: hydrogel microparticles, rosuvastatin calcium, polymerization, β-cyclodextrin solubilityhttps://www.dovepress.com/development-of-beta-cyclodextrin-based-hydrogel-microparticles-for-sol-peer-reviewed-article-DDDTHydrogel microparticlesrosuvastatin calciumpolymerizationβ-cyclodextrin solubility |
| spellingShingle | Sarfraz RM Ahmad M Mahmood A Akram MR Abrar A Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation Drug Design, Development and Therapy Hydrogel microparticles rosuvastatin calcium polymerization β-cyclodextrin solubility |
| title | Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation |
| title_full | Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation |
| title_fullStr | Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation |
| title_full_unstemmed | Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation |
| title_short | Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation |
| title_sort | development of beta cyclodextrin based hydrogel microparticles for solubility enhancement of rosuvastatin an in vitro and in vivo evaluation |
| topic | Hydrogel microparticles rosuvastatin calcium polymerization β-cyclodextrin solubility |
| url | https://www.dovepress.com/development-of-beta-cyclodextrin-based-hydrogel-microparticles-for-sol-peer-reviewed-article-DDDT |
| work_keys_str_mv | AT sarfrazrm developmentofbetacyclodextrinbasedhydrogelmicroparticlesforsolubilityenhancementofrosuvastatinaninvitroandinvivoevaluation AT ahmadm developmentofbetacyclodextrinbasedhydrogelmicroparticlesforsolubilityenhancementofrosuvastatinaninvitroandinvivoevaluation AT mahmooda developmentofbetacyclodextrinbasedhydrogelmicroparticlesforsolubilityenhancementofrosuvastatinaninvitroandinvivoevaluation AT akrammr developmentofbetacyclodextrinbasedhydrogelmicroparticlesforsolubilityenhancementofrosuvastatinaninvitroandinvivoevaluation AT abrara developmentofbetacyclodextrinbasedhydrogelmicroparticlesforsolubilityenhancementofrosuvastatinaninvitroandinvivoevaluation |