Nanoparticle formulation of amoxicillin
A nanoparticle, amoxicillin technology, applied in the field of amoxicillin nanoparticle formulations, can solve the problems of inability to achieve effective antimicrobial concentration, short residence time, etc.
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Embodiment 1
[0050] Embodiment 1. Preparation of amoxicillin nanoparticles
[0051] Glucosamine (10 mg from Sigma-Aldrich) was dissolved in water (1 mL) along with amoxicillin (3 mg from Sigma-Aldrich) at room temperature. If the polyglucosamine used is not completely water soluble, add sufficient amount of acetic acid (0.1%-2%) to increase water solubility. The anionic surfactant dioctyl sodium sulfosuccinate was then added to the solution with moderate stirring to a final concentration of 5% w / v and mineral or vegetable oil to a final concentration >75% v / v. The polyglucosamine solution is not miscible with oil and the surfactant acts to stabilize the polyglucosamine nanoparticles. Glutaraldehyde (from Alfa-Aesar) was then added to the mixture to a final concentration of 5%, followed by immediate mixing for 30 minutes to form an emulsification. During emulsification, crosslinking occurs and nanoparticles are formed. When the reaction had ceased, the particles were separated from the s...
Embodiment 2
[0052] Example 2. Nanoparticle Characterization
[0053]The nanoparticles of Example 1 were resuspended in water at a concentration of 1 mg / mL. The particle size and particle size distribution were measured by dynamic light scattering (DLS) using a Malvern Zetasizer (ZEN 3600). To further characterize the morphology, a drop of the nanoparticle suspension was placed on a silica wafer and then air dried overnight. The wafer with the dried sample on it was then coated with chromium and imaged by scanning electron microscopy (SEM).
[0054] Such as figure 2 The average hydrodynamic diameter of the particles is 324.6 nm and the polydispersity index (polydispersity index, PDI) is 0.2 ( figure 2 A). According to SEM, the dry powder exhibits particle morphology with an average diameter of about 300 nm, which is consistent with DLS measurements ( figure 2 B) Consistent.
Embodiment 3
[0055] Embodiment 3. Determination of amoxicillin loading rate
[0056] To measure the drug loading ratio (weight of drug / total weight of nanoparticles), amoxicillin-loaded nanoparticles were formulated following the same procedure described in Example 1, but using different initial drug amounts of 0.1, 1, 2.5 or 5 mg . 1 mg of dry nanoparticles were suspended using 15 mL of water. The suspension was stirred vigorously at 4°C for 12 hours to completely release the loaded drug. The suspension was then filtered through an Amicon filter tube with a molecular weight cutoff of 10 kDa. The amoxicillin concentration in the filtrate was measured and the drug loading was calculated.
[0057] Such as image 3 As shown in , the amoxicillin loading rate in nanoparticles increases with the initial concentration of amoxicillin. When the input concentration of amoxicillin was 0.1, 1, 2.5 and 5 mg / mL, the corresponding loading rates were determined to be 3.9%, 6.9%, 14.2% and 24.1%, resp...
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