Fabrication of PLA-Based Nanoneedle Patches Loaded with Transcutol-Modified Chitosan Nanoparticles for the Transdermal Delivery of Levofloxacin

Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches c...

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Published inMolecules (Basel, Switzerland) Vol. 29; no. 18; p. 4289
Main Authors Samiotaki, Christina, Koumentakou, Ioanna, Christodoulou, Evi, Bikiaris, Nikolaos D, Vlachou, Marilena, Karavas, Evangelos, Tourlouki, Konstantina, Kehagias, Nikolaos, Barmpalexis, Panagiotis
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 10.09.2024
MDPI
Subjects
Administration, Cutaneous
Animals
Anti-Bacterial Agents - administration & dosage
Anti-Bacterial Agents - chemistry
Chitosan - chemistry
Drug Carriers - chemistry
Drug Delivery Systems
Drug Liberation
drug release
Ethylene
Levofloxacin
Levofloxacin - administration & dosage
Levofloxacin - chemistry
nanoencapsulation
nanoneedles
Nanoparticles
Nanoparticles - chemistry
Particle Size
Permeability
Pharmaceuticals
poly(lactic acid) blends
Polyesters - chemistry
Polymers
Ratios
Skin
Skin - metabolism
Skin Absorption
Spectrum analysis
Toxicity
transdermal delivery
Transdermal medication
Transdermal Patch
Vibration
Greece
Japan
Germany
nanoneedles
nanoencapsulation
drug release
levofloxacin
transdermal delivery
poly(lactic acid) blends
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Abstract Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, / ), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%).
AbstractList Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, w/w), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%).Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, w/w), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%).
Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, w/w), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%).
Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, / ), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%).
Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, w / w ), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%).
Audience Academic
Author Vlachou, Marilena
Tourlouki, Konstantina
Bikiaris, Nikolaos D
Kehagias, Nikolaos
Koumentakou, Ioanna
Karavas, Evangelos
Barmpalexis, Panagiotis
Christodoulou, Evi
Samiotaki, Christina
AuthorAffiliation 1 Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece; christinasamiotaki@gmail.com (C.S.); iwanna.koumentakou@gmail.com (I.K.)
3 Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 15784 Athens, Greece; vlachou@pharm.uoa.gr
6 Institute of Nanoscience and Nanotechnology, NCSR Demokritos, 15341 Paraskevi, Greece; n.kehagias@inn.demokritos.gr
5 Nanotypos, Stivos, 57020 Thessaloniki, Greece; ktourlouki@nanotypos.com
2 Laboratory of Pharmaceutical Technology, Division of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece; nbikiaris@gmail.com
4 Pharmathen S.A., Pharmaceutical Industry, Dervenakion Str. 6, Pallini Attikis, 15351 Athens, Greece; ekaravas@pharmathen.gr
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Keywords nanoneedles
nanoencapsulation
drug release
levofloxacin
transdermal delivery
poly(lactic acid) blends
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Snippet Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However,...
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StartPage 4289
SubjectTerms Administration, Cutaneous
Animals
Anti-Bacterial Agents - administration & dosage
Anti-Bacterial Agents - chemistry
Chitosan - chemistry
Drug Carriers - chemistry
Drug Delivery Systems
Drug Liberation
drug release
Ethylene
Levofloxacin
Levofloxacin - administration & dosage
Levofloxacin - chemistry
nanoencapsulation
nanoneedles
Nanoparticles
Nanoparticles - chemistry
Particle Size
Permeability
Pharmaceuticals
poly(lactic acid) blends
Polyesters - chemistry
Polymers
Ratios
Skin
Skin - metabolism
Skin Absorption
Spectrum analysis
Toxicity
transdermal delivery
Transdermal medication
Transdermal Patch
Vibration
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Title Fabrication of PLA-Based Nanoneedle Patches Loaded with Transcutol-Modified Chitosan Nanoparticles for the Transdermal Delivery of Levofloxacin
URI https://www.ncbi.nlm.nih.gov/pubmed/39339284
https://www.proquest.com/docview/3110652323/abstract/
https://www.proquest.com/docview/3110913169/abstract/
https://pubmed.ncbi.nlm.nih.gov/PMC11433958
https://doaj.org/article/e2a8c83374914d6284305776fb0e7b98
Volume 29
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