Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability.
Stable solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) formulations to enhance the dissolution rates of poorly soluble drug spironolactone (SP) were being developed. Probe ultra-sonication method was used to prepare SLNs and NLCs. All NLCs contained stearic acid (solid lipid carrier) and oleic acid (liquid lipid content), whereas, SLNs were prepared and optimised by using the solid lipid only. The particles were characterised in terms of particle size analysis, thermal behaviour, morphology, stability and in vitro release. The zeta sizer data revealed that the increase in the concentration of oleic acid in the formulations reduced the mean particle size and the zeta potential. The increase in concentration of oleic acid from 0 to 30% (w/w) resulted in a higher entrapment efficiency. All nanoparticles were almost spherically shaped with an average particle size of about ∼170 nm. The DSC traces revealed that the presence of oleic acid in the NLC formulations resulted in a shift in the melting endotherms to a higher temperature. This could be attributed to a good long-term stability of the nanoparticles. The stability results showed that the particle size remained smaller in NLC compared to that of SLN formulations after 6 months at various temperatures. The dissolution study showed about a 5.1- to 7.2-fold increase in the release of the drug in 2 h compared to the raw drug. Comparing all nanoparticle formulations indicated that the NLC composition with a ratio of 70:30 (solid:liquid lipid) is the most suitable formulation with desired drug dissolution rates, entrapment efficiency and physical stability.
Pharmaceutical Sciences Research Centre, Mazandaran University of Medical Sciences, Sari, Iran.
H R
HR
Kelidari
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
M
M
Saeedi
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
J
J
Akbari
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
K
K
Morteza-Semnani
Drug applied Research Centre and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
H
H
Valizadeh
Pharmaceutics Research Laboratory, Arundel Building, School of Life Sciences, University of Sussex, Brighton, BN1 9QG, UK.
Mohammed
M
Maniruzzaman
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Ali
A
Farmoudeh
Pharmaceutics Research Laboratory, Arundel Building, School of Life Sciences, University of Sussex, Brighton, BN1 9QG, UK. a.nokhodchi@sussex.ac.uk.|Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. a.nokhodchi@sussex.ac.uk.
Ali
A
Nokhodchi
D004337:Drug Carriers; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004355:Drug Stability; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D012995:Solubility; D013148:Spironolactone / Q000737:chemistry / Q000494:pharmacology; D013229:Stearic Acids / Q000737:chemistry / Q000494:pharmacology
D004337:Drug Carriers; D013229:Stearic Acids; D013148:Spironolactone; C031183:stearic acid
drug release; solid lipid nanoparticles; spironolactone; stability