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Formulation and Characterization of Bioactive Agent Containing Nanodisks
Published on: March 17, 2023
Meloxicam-loaded Phospholipid/solutol® HS15 Based Mixed Nanomicelles: Preparation, Characterization, and in vitro
1Department of Pharmaceutics, Prin. K. M. Kundnani College of Pharmacy, Plot No. 23, Jote Joy Building, Rambhau Salgaonkar Marg, Cuffe Parade, Mumbai-400005, India.
Background:
Rheumatoid arthritis (RA) is a debilitating disease which results in joint destruction, mainly due to chronic inflammation and oxidative stress. Meloxicam (MLX) is a preferential cyclooxygenase-2 (COX-2) inhibitor with potential free radical scavenging activity. Mixed nanomicelles (NMs) of MLX can augment its antioxidant effects.
Objective:
The present study aims to prepare, characterize, and evaluate the in vitro antioxidant effects of MLX-loaded mixed nanomicelles (MLXNMs).
Method:
Conventional thin-film hydration method was employed to fabricate MLX-NMs. The formulations were characterized for particle size, zeta potential, entrapment efficiency (EE), and drug loading (DL). Additionally, the optimized formulation was characterized for small-angle neutron scattering (SANS), in vitro drug release, and morphology. MLX encapsulation in NMs was confirmed by Fourier Transform Infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), 1H nuclear magnetic resonance (NMR), and X-ray diffraction (XRD), studies. The cell uptake of sulforhodamine B (SRB)- labeled NMs was studied in RAW 264.7 cells. The in vitro antioxidant activity of optimized MLX-NMs was studied by different antioxidant assays.
Results:
The optimized MLX-NMs exhibited average size and zeta potential of 88 ± 42 nm and -47.4 ± 16.2 mV, respectively. The EE and DL of MLX were 94.13 ± 1.01 % and 4.20 ± 0.05 %, respectively. Morphology studies confirmed the oblate ellipsoidal shape of MLXNMs. The in vitro release study exhibited a biphasic release pattern. MLX encapsulation into the micelle core was confirmed by FTIR, DSC, 1H NMR, and XRD studies. Additionally, SRB-labeled NMs demonstrated efficient in vitro cell uptake in RAW 264.7 cells. Furthermore, in vitro antioxidant studies exhibited superior free radical scavenging activity of MLXNMs as compared to free MLX.
Conclusion:
The NMs potentiate the in vitro antioxidant effects of MLX.
Insights
Mixed nanomicelles (NMs) loaded with Meloxicam (MLX) were developed to enhance antioxidant effects for rheumatoid arthritis (RA). These MLX-NMs demonstrated superior free radical scavenging activity compared to free MLX in vitro.
Area of Science:
- Nanotechnology
- Materials Science
- Pharmacology
Background:
- Rheumatoid arthritis (RA) involves joint destruction driven by chronic inflammation and oxidative stress.
- Meloxicam (MLX), a COX-2 inhibitor, possesses free radical scavenging properties.
- Mixed nanomicelles (NMs) can enhance the antioxidant capacity of MLX.
Purpose of the Study:
- To prepare and characterize MLX-loaded mixed nanomicelles (MLX-NMs).
- To evaluate the in vitro antioxidant effects of MLX-NMs.
Main Methods:
- Fabrication of MLX-NMs using the thin-film hydration method.
- Characterization of particle size, zeta potential, entrapment efficiency (EE), and drug loading (DL).
- Confirmation of MLX encapsulation using FTIR, DSC, 1H NMR, and XRD; evaluation of in vitro antioxidant activity and cell uptake.
Main Results:
- Optimized MLX-NMs showed an average size of 88 ± 42 nm and zeta potential of -47.4 ± 16.2 mV.
- High EE (94.13 ± 1.01%) and DL (4.20 ± 0.05%) were achieved.
- MLX-NMs exhibited enhanced in vitro antioxidant activity and efficient cell uptake compared to free MLX.
Conclusions:
- The developed nanomicelles effectively potentiate the in vitro antioxidant effects of Meloxicam.
- MLX-NMs represent a promising approach to augment the antioxidant therapy for conditions like rheumatoid arthritis.
