Nanoparticles Challenges for Antibiotic Drug Delivery using Penicillin as a Model Drug Dr B BBarik Professor Dept of Pharmaceutics Mohammed M Safhi SMSivakumar Aamena ID: 449773
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Chitosan Nanoparticles - Challenges for Antibiotic Drug Delivery using Penicillin as a Model Drug
Dr
. B. B.BarikProfessor, Dept. of PharmaceuticsMohammed M. Safhi, S.M.Sivakumar, Aamena Jabeen, Foziyah Zakir & Farah Islam College of Pharmacy, Jazan University, Kingdom of Saudi Arabia. E-mail: bbbarik2003@gmail.com
5
th
International Conference and Exhibition on
Pharmaceutics & Novel Drug Delivery Systems
March 16-18, 2015
Crowne
Plaza, Dubai, UAE
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INTRODUCTIONAntibiotic resistance is one of the major health and economic
problems worldwide eroding the discovery of antibiotics and their application to clinical medicine.
It has been estimated that each year in US, approximately 2 million people get infected with antibiotic resistance bacteria and 23,000 die as a result of these infections . Resistance to penicillin is well recognized in Staphylococcus aureus and Staphylococcus epidermidis .Use of nanoparticles for antibiotic delivery is increasing due to increased prevalence of antibiotic resistant bacterial strains.Slide3
Antibiotic ResistanceSlide4Slide5Slide6
WHY NANOPARTICLES AND WHY CHITOSAN
?
Nanoparticles can easily bypass efflux mechanism, particularly chitosan nanopartilcles because chitosan is highly poly cationic can easily bind with anionic microbial cells. Efflux mechanism: Membrane proteins that export antibiotics from the cell and maintain their low intracellular concentrations. Outer membrane permeability: An asymmetric bilayer: the phospholipid form the inner leaflet and the lipopolysaccharides (LPS) form the outer leaflet, provides a formidable barrier that must be overcome by drugs.Slide7Slide8Slide9Slide10
ObjectiveThe objective of this study was to formulate and characterize chitosan nanoparticles of penicillin G to improve the bioavailability and prevent drug resistance.Slide11
Method
Ionic
gelation technique was used to encapsulate penicillin G in chitosan nanoparticles. The anti bacterial efficacy of penicillin-loaded chitosan nanoparticles were evaluated against five bacterial strains namely:Staphylococcus aureus Streptococcus pyogenes
Bacillus
subtilis
Escherichia coli and Klebsiella planticola The antibacterial effect of penicillin nanoparticles was compared with conventional penicillin drug.Slide12
Preparation of chitosan
nanoparticle of penicillin G1% w/v chitosan solution was prepared with 1% v/v glacial acetic acid having pH 4. The pH was increased to 6 by adding 1ml of 1N NaOH. The chitosan gel was homogenized at 3600 rpm for 30 minutesDuring homogenization 1 ml of 1% w/v of penicillin G was added. Sonication was done for 30 seconds at pre determined time interval.500
μl
of formaldehyde was added drop by drop and homogenization was continued for one hour.
The penicillin loaded
nanoparticles were washed & dried.Slide13
Prepartion of pencillin –
chitosan
nanoparticlesIONIC GELLATION TECHNIQUESlide14
Chitosan
Chitosan
cross linkingSlide15
Characterisation of
nanoparticles
Morphology The nanoparticles were observed under TEM with an accelerating voltage of 100 kvZeta potential, Particle size and PDIThe zeta potential, size and PDI of penicillin loaded chitosan nanoparticles were measured by using Nano – ZS zeta sizer, Malvern Instruments, UK.
In vitro release profile
2 ml of penicillin loaded
chitosan
nanoparticles were taken in 50 ml of phosphate buffer of pH 6.0 placed in a beaker and stirred in a magnetic stirrer at 50 rpm for 48 hrs at a temperature of 25ºC. The samples were withdrawn, centrifused and assayed spectrophotometrically at 208 nm.Slide16
Assessment of antibacterial activity
Following five bacterial strains
were used: Staphylococcus aureus, Streptococcus pyogenes, Bacillus subtilis,Escheriachia coli and Klebsiella planticola
The MIC was determined in Nutrient Broth using two-fold serial dilutions of
chitosan
nanoparticles with initial bacterial inoculums of 10-6 CFU and the time and temperature of incubation being 24 hours and 370C, respectively.Slide17
Morphology and Size
TEM analysis Slide18
Zeta potential, Particle size
and
pdi:
Polymer
Cross linker
Before sonication
After
sonication
Size (nm)
PdI
Zeta
potntial
Sonication
time
(Sec)
Size (nm)
PdI
Zeta
potntial
0.1%
250 µl
644.2
1.00
35.4 mV
10
497.2
0.59
55.4
0.1%
500 µl
585.9
0.63
42.4
15
401.1
0.48
62.8
0.1%
1000 µl
1057
0.7
37.3
20
3
0.3
52.3
0.1%
1500 µl
1167
0.8
33.7
25
661
0.51
46.8Slide19
In vitro
release Slide20
Anti bacterial studies Slide21
CONCLUSION
This work confirms that ionic
gelation technique is a successful method to encapsulate penicillin in chitosan nanoparticles. Penicillin is released in sustained manner from chitosan nanoparticle.It showed better microbial action than conventional penicillin.Slide22
CDC.Active Bacterial Core Surveillance Methodology (2012).http://www.cdc.gov/abcs/ index.htmlKimberlin, C., Khalid, F., Hariri, A. Resistance of staphylococci to penicillin-G and cloxacillin. Pahlavi Med J. 9(2),1978, 182 - 192. Guo
, L., Yang, S. Synthesis and Characterization of Poly(vinylpyrrolidone)-Modified Zinc Oxide nanoparticles. Chem. Mater. 12, 2000, 2268-2274
Pertha, S., Amit, K.G., Goutam, R. Formulation and evaluation of chitosan based ampicillin trihydrate nanoparticles. Trop J Pharm Res. 9(5), 2010 : 483 – 488. Sarmento, B., Riberio A, Veiga F, Sampaio P, Neufeld R, Ferreira D. Alginate/Chitosan nanoparticles are effective for oral insulin delivery. Pharmaceutical Research. 2007; 24(12): 2198 – 2206ReferencesSlide23
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