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A potential in situ gel formulation loaded with novel fabricated poly(lactide-co-glycolide) nanoparticles for enhancing and sustaining the ophthalmic delivery of ketoconazole
- Source :
- International Journal of Nanomedicine
- Publication Year :
- 2017
- Publisher :
- Informa UK Limited, 2017.
-
Abstract
- Tarek Abdelnapy Ahmed,1,2 Bader M Aljaeid1 1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo,Egypt Abstract: Oral ketoconazole therapy is commonly associated with serious hepatotoxicity. Improving ocular drug delivery could be sufficient to treat eye fungal infections. The purpose of this study was to develop optimized ketoconazole poly(lactide-co-glycolide) nanoparticles (NPs) with subsequent loading into in situ gel (ISG) formulation for ophthalmic drug delivery. Three formulation factors were optimized for their effect on particle size (Y1) and entrapment efficiency (Y2) utilizing central composite experimental design. Interaction among components was studied using differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy. Ketoconazole crystalline state was studied using X-ray powder diffraction. Six different polymeric ISG formulations were prepared and loaded with either optimized NPs or a pure drug. The prepared ISG formulations were characterized for invitro gelation, drug release and antifungal activity. The permeation through human epithelial cell line was also investigated. The results revealed that all the studied formulation parameters significantly affected Y1 and Y2 of the developed NPs. DSC and FTIR studies illustrated compatibility among NP components, while there was a change from the crystalline state to the amorphous state of the NPs. The in vitro release from the ISG formulations loaded with drug NPs showed sustained and enhanced drug release compared to pure drug formulations. In addition, ISG loaded with NPs showed enhanced anti-fungal activity compared to pure drug formulations. Alginate–chitosan ISG formulation loaded with optimized ketoconazole NPs illustrated higher drug permeation through epithelial cell lines and is considered as an effective ophthalmic drug delivery in the treatment of fungal eye infections. Keywords: ketoconazole, PLGA, nanoparticles, ISG, ophthalmic delivery
- Subjects :
- Chemistry, Pharmaceutical
Pharmaceutical Science
Nanoparticle
02 engineering and technology
030226 pharmacology & pharmacy
Cornea
Diffusion
chemistry.chemical_compound
Drug Delivery Systems
0302 clinical medicine
Polylactic Acid-Polyglycolic Acid Copolymer
X-Ray Diffraction
International Journal of Nanomedicine
Spectroscopy, Fourier Transform Infrared
Drug Discovery
Original Research
media_common
Calorimetry, Differential Scanning
PLGA
General Medicine
Permeation
021001 nanoscience & nanotechnology
Drug delivery
Ketoconazole
0210 nano-technology
medicine.drug
Drug
Materials science
media_common.quotation_subject
ketoconazole
Biophysics
Bioengineering
Nanotechnology
ISG
Biomaterials
ophthalmic delivery
03 medical and health sciences
Differential scanning calorimetry
medicine
Humans
Lactic Acid
Particle Size
Fourier transform infrared spectroscopy
Organic Chemistry
technology, industry, and agriculture
Drug Liberation
chemistry
Polyvinyl Alcohol
Nanoparticles
Gels
Polyglycolic Acid
Nuclear chemistry
Subjects
Details
- ISSN :
- 11782013
- Volume :
- 12
- Database :
- OpenAIRE
- Journal :
- International Journal of Nanomedicine
- Accession number :
- edsair.doi.dedup.....76fb1453a94762a9033e2373feb706cf
- Full Text :
- https://doi.org/10.2147/ijn.s131850