Influence of Solvent Evaporation Technique Parameters on Diameter of Submicron Lamivudine-Poly-ε-Caprolactone Conjugate Particles

Abstract

The size of active pharmaceutical ingredient carrier is one of the key properties considered during design of submicron drug delivery systems. Particle diameter may determine drug biodistribution, cellular uptake, and elimination path. Solvent evaporation technique is a flexible method of particle preparation, in which various macromolecules and drugs may be employed. Parameters of emulsion obtained as first step of particle preparation are crucial in terms of particle size, drug loading, and morphology. The aim of the study was to investigate the influence of emulsion preparation parameters on diameter of resulting particles. Impact of surfactant type and concentration, homogenization time, homogenization rate, phase ratio, and conjugate concentration were evaluated. Model drug lamivudine was covalently bound to polymer and applied in solvent evaporation method in order to overcome issues related to drug loading and provide method-independent incorporation. Synthesized drug–polymer conjugate and obtained particles were evaluated via dynamic light scattering, chromatography, scanning electron microscopy, and spectroscopic methods. Covalent bonding between drug and polymeric chain was confirmed, estimated drug content per milligram of conjugate was 19 μg. Among employed colloid stabilizer, poly(vinyl alcohol) was proven to be most effective. Homogenization rate and surfactant concentration were identified as crucial parameters in terms of particle diameter control.

Effect of Oxaliplatin-Loaded Poly (d,l-Lactide-co-Glycolic Acid) (PLGA) Nanoparticles Combined with Retinoic Acid and Cholesterol on Apoptosis, Drug Resistance, and Metastasis Factors of Colorectal Cancer

“…In addition, PVA acted as an effective stabilization and the PVA surfactant molecules allowed us to achieve small particle size and narrow size distribution. A very low concentrations of PVA remained on the surface of nanoparticles [29]. The solution was transferred to a new vial that contained an air-dried solution of 20 mg CHO (Avati Polar Lipids, Alabaster, AL, USA), dissolved in 0.4 mL of chloroform, and homogenized by sonication.…”

Alginate Nanoformulation: Influence of Process and Selected Variables

“…The resulted emulsion is then transferred under the same condition to the aqueous phase of surfactant to produce a double emulsion (w/o/w) ( Figure 4 B) [ 8 ]. Under the same condition, nanoparticles are hardened after solvent removal, while the physical and chemical properties of the synthesized nanoparticle can be tuned by tailoring the emulsion properties, such as surfactant concentration/type, o/w phase ratio, polymer concentration and evaporation rate as well as processing parameters, including agitation rate and time, geometry of homogenizing tip, and shape and volume of homogenizer vessel [ 75 , 76 ].…”

Nanomaterials Designed for Antiviral Drug Delivery Transport across Biological Barriers

“…Lamivudine-LAM, a water-soluble drug with two main drawbacks: its half-life is only 2 h and has a deficient bioavailability, especially in paediatric patients (68%) [177]. LAM has been included in NPs based on poly(ε-caprolactone)-PCL [178,179], poly lactic-co-glycolic acid-PLGA [141], chitosan and sodium alginate [180], Eudragit E100 [177]. The physico-chemical characterization of the obtained NPs has shown an adequate size of the NPs and a good stability.…”