Development and evaluation of Terbutaline Sulphate loaded-biodegradable microspheres for pulmonary delivery

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dc.contributor.authorRehab Abdallah, Mohammed Ahmed
dc.date.accessioned2014-11-14T07:57:12Z
dc.date.available2014-11-14T07:57:12Z
dc.date.issued2007
dc.descriptionMasteren_US
dc.description.abstractSustained-release terbutaline sulphate (TBS) microspheres were developed using PLA R 203H and PLGA RG 504H polymers. The microspheres were prepared using the double emulsion solvent evaporation method and the amount of TBS entrapped in the microspheres was determined by UV spectrometry. The influence of surfactants (PVA and sodium oleate) and gelatin in the external phase and the pH in internal phase on the physical characteristics of the microspheres were investigated. PVA (0.5 and 5%), sodium oleate (0.1 and 0.5%) and pH (4, 5.8 and 7.4) were found to influence the physical characteristics (size, yield, drug loading and entrapment efficiency) of the microspheres. Conversely, gelatin (25, 50 and 100 mg) had no effect on the physical characteristics of both PLA and PLGA microspheres. At optimum level (PVA 0.5%, sodium oleate 0.1% and pH 7.4) the drug loading, entrapment efficiency, yield and mean particles size of PLA were 0.85%, 34.99 %, 87.11% and 6.55 μm while that of PLGA were 0.76%, 31.17%, 84.52% and 8.64 μm respectively. The DSC thermal profiles revealed that the Tg of PLA and PLGA microspheres shifted to a lower value when TBS incorporated into microspheres. Moreover, the FTIR spectra also showed a shift in the characteristic peak of TBS in microspheres. This indicates that molecular interaction had occurred between TBS and polymers within the microspheres. The scanning electron microscope revealed that the surface structure of PLA was more porous than that of PLGA microspheres. Furthermore, the release of drug from PLA microspheres was faster than from PLGA microspheres. An addition of gelatin to the formulation was found to prolong the release of drug from the microspheres. Drug release at the initial rapid phase (6 h) from PLA and PLGA without gelatin was 76.31% and 55.4% respectively while the remaining amount was released within 24 h and 72 h respectively. In contrast, drug release at the initial rapid phase from PLA and PLGA with gelatin was 35.4% and 22.4% respectively while the remaining amount was released within 144 h and >144 h respectively. The drug release from both PLA and PLGA microspheres without gelatin fitted first order release kinetics model. However, drug release from PLA and PLGA with gelatin followed the Higuchi and biexponential first order release kinetics models respectively. The mean aerosols size (MMAD) of rehydrated PLA (2.53 μm) and rehydrated PLGA (3.50 μm) generated using nebulizer were smaller than the MMAD of PLA (11.10 μm) and PLGA (11.47 μm) produced by a Rotahaler. In addition, the fine particle fraction (FPF) of PLA (49.54%) and PLGA (37.50%) aerosolized by a nebulizer were higher than the FPF of PLA (11.89%) and PLGA (10.57%) produced by a Rotahaler. In conclusion, TBS- loaded PLA microspheres is a promising candidate for pulmonary delivery of sustained-release TBS using a nebulizer.en_US
dc.identifier.urihttp://hdl.handle.net/123456789/523
dc.language.isoenen_US
dc.subjectPharmaceutical scienceen_US
dc.subjectTerbutaline Sulphateen_US
dc.subjectPulmonary Deliveryen_US
dc.titleDevelopment and evaluation of Terbutaline Sulphate loaded-biodegradable microspheres for pulmonary deliveryen_US
dc.typeThesisen_US
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