Abstract
Aim
Meropenem hydrochloride (MpM)-loaded nanostructured lipid carriers were designed for the effective management of skin infection caused by Staphylococcus aureus via topical route. The solvent evaporation tactic was preferred to develop nanostructured lipid carriers (NLCs). Stearic acid was used as a solid fatty acid; oleic acid was used as liquid fatty acid and Tween 80 as a surfactant. The Staphylococcus aureus burden was analyzed by pharmacodynamic studies. The skin retention was analyzed by fluorescence microscopy. Spherical shape of NLCs was confirmed by TEM. The optimum particle size of the MpM-NLCs was ~ 126.5 ± 0.9 nm with 79.1 ± 2.3% entrapment (EE) and 0.967 mV zeta potential. The in vitro release studies revealed 81.5 ± 3.1% release of drug in 48 h, while the pure drug was almost completely released (98.4 ± 1.4%) within 24 h confirming the potential of NLCs for sustained topical drug delivery. Skin permeation study also revealed better permeation of drug from NLCs than of plain drug. The prepared MpM-NLCs when stored at 4 ± 2°C for 90 days were found to be more stable when the formulation was stored at 28 ± 2°C. The S. aureus burden was analyzed by evaluating the zone of inhibition (ZOI). The ZOI of MpM alone and MpM-NLC gel was measured and compared with that of the control group. The MpM was found significantly effective when its gel was prepared with NLCs because of its enhanced adhesion property occlusion and ability to sustain release. In overall, the study’s outcomes validated the relevance of NLC’s composition as a vehicle for topical MpM administration in skin diseases caused by Staphylococcus aureus.
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Abbreviations
- BBD:
-
Box-Behnken design
- CLSM:
-
Confocal laser scanning microscopic
- DOE:
-
Design of experiment
- EE:
-
Entrapment efficiency
- FITC:
-
Fluorescein isothiocyanate
- MpM:
-
Meropenem
- NLCs:
-
Nanostructured lipid carriers
- SSTI:
-
Skin and soft tissue infections
- TEM:
-
Transmission electron microscope
- USFDA:
-
US Food and Drug Administration
- WHO:
-
World Health Organization
- ZOI:
-
Zone of inhibition
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Acknowledgements
All the authors are thankful to Bhagyoday Tirth Pharmacy College, Sagar, Madhya Pradesh, for providing laboratory facilities, and Dr. H.S. Gour Central University, Sagar, Madhya Pradesh, for TEM facility.
Funding
This study was supported by a Junior Research fellowship from the AICTE, New Delhi.
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KS, SKP: experimental work, drafting.
AM: designing of experiments and performing CLSM studies, in vivo studies, drafting, editing.
RJ: in vivo pharmacodynamic studies, designing of experiments, editing and proof reading before submission.
AJ: conceptu; guidance in experiments, drafting, editing.
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Rajpoot, K., Prajapati, S.K., Malaiya, A. et al. Meropenem-Loaded Nanostructured Lipid Carriers For Skin and Soft Tissue Infection Caused by Staphylococcus aureus: Formulation, Design, and Evaluation. AAPS PharmSciTech 23, 241 (2022). https://doi.org/10.1208/s12249-022-02381-y
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DOI: https://doi.org/10.1208/s12249-022-02381-y