Mandeep Singh1, Ana Guzman-Aranguez2, Afzal Hussain3, Cheerneni S Srinivas4, Indu P Kaur1. 1. University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India. 2. Department of Biochemistry & Molecular Biology, Faculty of Optics & Optometry, Universidad Complutense de Madrid, Madrid 28040, Spain. 3. Department of Pharmaceutical Sciences & Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835215, India. 4. Department of Chemical Sciences, Indian Institute of Science Education & Research Mohali, Punjab 140306, India.
Abstract
AIM: Evaluation of solid lipid nanoparticles (SLNs) for ocular delivery of isoniazid (INH). MATERIALS & METHODS: INH-SLNs were characterized for morphological, thermal, crystalline and nuclear magnetic resonance properties. In vitro release and ex vivo corneal permeability of INH-SLNs was also evaluated. Proof-of-concept uptake studies were performed in corneal and conjunctival cell lines and in vivo in rat eye using fluorescein-labeled SLNs. Antimycobacterial activity of INH-SLNs was confirmed. In vivo aqueous humor pharmacokinetics, toxicity and tolerance was performed in rabbit/rat eye. RESULTS: INH-SLNs showed extended release (48 h), enhanced corneal permeability (1.6-times), five-times lower MIC, significant in vitro and in vivo uptake of fluorescein-labeled SLNs, 4.2-times ocular bioavailability (area under the curve) and in vivo acute and repeat dose safety. CONCLUSION: INH-SLNs are an effective ocular delivery system.
AIM: Evaluation of solid lipid nanoparticles (SLNs) for ocular delivery of isoniazid (INH). MATERIALS & METHODS: INH-SLNs were characterized for morphological, thermal, crystalline and nuclear magnetic resonance properties. In vitro release and ex vivo corneal permeability of INH-SLNs was also evaluated. Proof-of-concept uptake studies were performed in corneal and conjunctival cell lines and in vivo in rat eye using fluorescein-labeled SLNs. Antimycobacterial activity of INH-SLNs was confirmed. In vivo aqueous humor pharmacokinetics, toxicity and tolerance was performed in rabbit/rat eye. RESULTS: INH-SLNs showed extended release (48 h), enhanced corneal permeability (1.6-times), five-times lower MIC, significant in vitro and in vivo uptake of fluorescein-labeled SLNs, 4.2-times ocular bioavailability (area under the curve) and in vivo acute and repeat dose safety. CONCLUSION: INH-SLNs are an effective ocular delivery system.
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