High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection

Antibiotic treatment of orthopaedic infection is complicated by systemic toxicity and the need of effective therapeutic concentration necessary to ensure optimum killing of bacteria. To overcome the problem of systemic toxicity and to achieve a high initial release followed by sustained release of a...

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Main Authors:	Harun Ismail, Ahmad Fahmi, Doolaanea, Abd Monem, Awang, Mohamed, Mohamed, Farahidah
Format:	Article
Language:	English
Published:	Academic Sciences 2012
Subjects:	RS Pharmacy and materia medica
Online Access:	http://irep.iium.edu.my/25825/ http://irep.iium.edu.my/25825/ http://irep.iium.edu.my/25825/1/High_burst_release_gentamicin_formulated_as_PLGAmicrospheres.pdf

id	iium-25825
recordtype	eprints
spelling	iium-258252012-09-24T06:12:41Z http://irep.iium.edu.my/25825/ High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection Harun Ismail, Ahmad Fahmi Doolaanea, Abd Monem Awang, Mohamed Mohamed, Farahidah RS Pharmacy and materia medica Antibiotic treatment of orthopaedic infection is complicated by systemic toxicity and the need of effective therapeutic concentration necessary to ensure optimum killing of bacteria. To overcome the problem of systemic toxicity and to achieve a high initial release followed by sustained release of antibiotics, a new method of delivering gentamicin is attempted by encapsulating gentamicin into PLGA using multiple emulsion, solvent-evaporation method. Gentamicin was first extracted from the microspheres and quantified using ninhydrin assay before the concentration was measured using UV spectrophotometer. Gentamicin efficacy after encapsulation was preserved when CTAB (83.51 ± 1.42%) and low molecular weight (LMW) PLGA (82.38 ± 9.08%) were used as indicated by drug loading efficiency of more than 80% in the disc-diffusion assay. LMW PLGA enabled high burst release (~90%) of gentamicin within the first 10 hours corresponding to zone inhibition of 13.78 ± 0.86 mm, only 30% smaller than the positive control (10 mg/ml gentamicin). The effects of Tg Keywords: Micro particles, Gentamicin; Surfactant, PLGA, Controlled-release and molecular weight rather than surfactant types influence the initial burst release. The in vitro release profile suggests that by having a mixture of various PLGA microspheres in one dosage implant system, the high burst release can be sustained within therapeutic concentration for a prolonged period (> 1 months). This biodegradable delivery system does not entail another surgery to remove the implant hence reducing the high treatment cost usually associated with the non-biodegradable proprietary gentamicin-polymethyl-methacrylate (PMMA) beads currently in use. Academic Sciences 2012-09 Article PeerReviewed application/pdf en http://irep.iium.edu.my/25825/1/High_burst_release_gentamicin_formulated_as_PLGAmicrospheres.pdf Harun Ismail, Ahmad Fahmi and Doolaanea, Abd Monem and Awang, Mohamed and Mohamed, Farahidah (2012) High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection. International Journal of Pharmacy and Pharmaceutical Sciences, 4 (supp.4). pp. 685-691. ISSN 0975-1491 http://www.ijppsjournal.com/Vol4Suppl4/4819.pdf
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
language	English
topic	RS Pharmacy and materia medica
spellingShingle	RS Pharmacy and materia medica Harun Ismail, Ahmad Fahmi Doolaanea, Abd Monem Awang, Mohamed Mohamed, Farahidah High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection
description	Antibiotic treatment of orthopaedic infection is complicated by systemic toxicity and the need of effective therapeutic concentration necessary to ensure optimum killing of bacteria. To overcome the problem of systemic toxicity and to achieve a high initial release followed by sustained release of antibiotics, a new method of delivering gentamicin is attempted by encapsulating gentamicin into PLGA using multiple emulsion, solvent-evaporation method. Gentamicin was first extracted from the microspheres and quantified using ninhydrin assay before the concentration was measured using UV spectrophotometer. Gentamicin efficacy after encapsulation was preserved when CTAB (83.51 ± 1.42%) and low molecular weight (LMW) PLGA (82.38 ± 9.08%) were used as indicated by drug loading efficiency of more than 80% in the disc-diffusion assay. LMW PLGA enabled high burst release (~90%) of gentamicin within the first 10 hours corresponding to zone inhibition of 13.78 ± 0.86 mm, only 30% smaller than the positive control (10 mg/ml gentamicin). The effects of Tg Keywords: Micro particles, Gentamicin; Surfactant, PLGA, Controlled-release and molecular weight rather than surfactant types influence the initial burst release. The in vitro release profile suggests that by having a mixture of various PLGA microspheres in one dosage implant system, the high burst release can be sustained within therapeutic concentration for a prolonged period (> 1 months). This biodegradable delivery system does not entail another surgery to remove the implant hence reducing the high treatment cost usually associated with the non-biodegradable proprietary gentamicin-polymethyl-methacrylate (PMMA) beads currently in use.
format	Article
author	Harun Ismail, Ahmad Fahmi Doolaanea, Abd Monem Awang, Mohamed Mohamed, Farahidah
author_facet	Harun Ismail, Ahmad Fahmi Doolaanea, Abd Monem Awang, Mohamed Mohamed, Farahidah
author_sort	Harun Ismail, Ahmad Fahmi
title	High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection
title_short	High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection
title_full	High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection
title_fullStr	High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection
title_full_unstemmed	High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection
title_sort	high initial burst release of gentamicin formulated as plga microspheres implant for treating orthopaedic infection
publisher	Academic Sciences
publishDate	2012
url	http://irep.iium.edu.my/25825/ http://irep.iium.edu.my/25825/ http://irep.iium.edu.my/25825/1/High_burst_release_gentamicin_formulated_as_PLGAmicrospheres.pdf
first_indexed	2023-09-18T20:38:29Z
last_indexed	2023-09-18T20:38:29Z
_version_	1777409206246178816

High initial burst release of gentamicin formulated as PLGA microspheres implant for treating orthopaedic infection

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