PMID- 24874603
OWN - NLM
STAT- MEDLINE
DCOM- 20150707
LR  - 20211021
IS  - 1573-904X (Electronic)
IS  - 0724-8741 (Print)
IS  - 0724-8741 (Linking)
VI  - 31
IP  - 12
DP  - 2014 Dec
TI  - Effects of antibiotic physicochemical properties on their release kinetics from 
      biodegradable polymer microparticles.
PG  - 3379-89
LID - 10.1007/s11095-014-1427-y [doi]
AB  - PURPOSE: This study investigated the effects of the physicochemical properties of 
      antibiotics on the morphology, loading efficiency, size, release kinetics, and 
      antibiotic efficacy of loaded poly(DL-lactic-co-glycolic acid) (PLGA) 
      microparticles (MPs) at different loading percentages. METHODS: Cefazolin, 
      ciprofloxacin, clindamycin, colistin, doxycycline, and vancomycin were loaded at 
      10 and 20 wt% into PLGA MPs using a water-in-oil-in water double emulsion 
      fabrication protocol. Microparticle morphology, size, loading efficiency, release 
      kinetics, and antibiotic efficacy were assessed. RESULTS: The results from this 
      study demonstrate that the chemical nature of loaded antibiotics, especially 
      charge and molecular weight, influence the incorporation into and release of 
      antibiotics from PLGA MPs. Drugs with molecular weights less than 600 Da 
      displayed biphasic release while those with molecular weights greater than 
      1,000 Da displayed triphasic release kinetics. Large molecular weight drugs also 
      had a longer delay before release than smaller molecular weight drugs. The 
      negatively charged antibiotic cefazolin had lower loading efficiency than 
      positively charged antibiotics. Microparticle size appeared to be mainly 
      controlled by fabrication parameters, and partition and solubility coefficients 
      did not appear to have an obvious effect on loading efficiency or release. 
      Released antibiotics maintained their efficacy against susceptible strains over 
      the duration of release. Duration of release varied between 17 and 49 days based 
      on the type of antibiotic loaded. CONCLUSIONS: The data from this study indicate 
      that the chemical nature of antibiotics affects properties of antibiotic-loaded 
      PLGA MPs and allows for general prediction of loading and release kinetics.
FAU - Shah, Sarita R
AU  - Shah SR
AD  - Department of Bioengineering, Rice University, MS-142, 6100 Main St., Houston, 
      Texas, 77005, USA.
FAU - Henslee, Allan M
AU  - Henslee AM
FAU - Spicer, Patrick P
AU  - Spicer PP
FAU - Yokota, Shun
AU  - Yokota S
FAU - Petrichenko, Sophia
AU  - Petrichenko S
FAU - Allahabadi, Sachin
AU  - Allahabadi S
FAU - Bennett, George N
AU  - Bennett GN
FAU - Wong, Mark E
AU  - Wong ME
FAU - Kasper, F Kurtis
AU  - Kasper FK
FAU - Mikos, Antonios G
AU  - Mikos AG
LA  - eng
GR  - T32 GM007330/GM/NIGMS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20140530
PL  - United States
TA  - Pharm Res
JT  - Pharmaceutical research
JID - 8406521
RN  - 0 (Anti-Bacterial Agents)
RN  - 0 (Polymers)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
SB  - IM
MH  - Anti-Bacterial Agents/administration & dosage/*chemistry/pharmacology
MH  - Bacteria/drug effects
MH  - Chemistry, Pharmaceutical
MH  - Kinetics
MH  - Lactic Acid
MH  - Microbial Sensitivity Tests
MH  - Microscopy, Electron, Scanning
MH  - Molecular Weight
MH  - Nanoparticles
MH  - Particle Size
MH  - Polyglycolic Acid
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Polymers
MH  - Solubility
PMC - PMC4225168
MID - NIHMS600558
EDAT- 2014/05/31 06:00
MHDA- 2015/07/08 06:00
PMCR- 2015/12/01
CRDT- 2014/05/31 06:00
PHST- 2014/03/25 00:00 [received]
PHST- 2014/05/12 00:00 [accepted]
PHST- 2014/05/31 06:00 [entrez]
PHST- 2014/05/31 06:00 [pubmed]
PHST- 2015/07/08 06:00 [medline]
PHST- 2015/12/01 00:00 [pmc-release]
AID - 10.1007/s11095-014-1427-y [doi]
PST - ppublish
SO  - Pharm Res. 2014 Dec;31(12):3379-89. doi: 10.1007/s11095-014-1427-y. Epub 2014 May 
      30.