Article

Study of the Effect of Formulation Parameters/Variables to Control the Nanoencapsulation of Hydrophilic Drug via Double Emulsion Technique

Université de Lyon, F-69622, Lyon, France.
Journal of Biomedical Nanotechnology (Impact Factor: 5.34). 04/2011; 7(2):255-62. DOI: 10.1166/jbn.2011.1279
Source: PubMed

ABSTRACT

Preparation of biodegradable nanoparticles containing active molecule is now taking much attention of researchers. The aim of the present work is to achieve the nanosize particles for the first time by double emulsion (W1/O/W2,) evaporation method to encapsulate hydrophilic substance using high performance stirring apparatus. A fluorescent stable hydrophilic agent (Stilbene derivative) was used as a model drug to be encapsulated. For this purpose, PCL (polycaprolactone) was chosen as polymer in this study. Several kinds of stabilizers [triton-405, tween 80, poloxamer, PVP (polyvinylpyrrolidone), PEG (poly ethylene glycol) & PVA (poly vinyl alcohol)] were investigated and the results indicate that the PVA (0.5% concentration) leads to the most stable double emulsion with the particle size in nano range. Different parameters affecting the size of particles have been studied such as stirring time (for 1st and 2nd emulsion), stirring speed (for 1st and 2nd emulsion), polymer and stabilizer concentrations etc. After duration of one month, the encapsulation efficiency of obtained particles was estimated using U.V. analysis. Transmission Electron Microscopy (TEM) showed that the prepared particles were spherical in shape. The size and size distribution were found to be submicron and ranging from 150 to 400 nm.

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    • "However, the hydrophilic ofloxacin always results in the low drug loading efficiency in hydrophobic polymeric drug carriers such as polylactide-glycoside and also faces high burst release [18, 19]. Approaches used to prevent the hydrophilic drugs partitioning to the external aqueous phase during emulsification and hardening procedure include presaturation of external phase with drug, altering the aqueous phase pH and using more water-miscible solvents [23–27]. But the efficiency of all these endeavors is still needed to be improved. "
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    ABSTRACT: We use hydrophobic poly(lactic-co-glycolic) acid (PLGA) to encapsulate hydrophilic ofloxacin to form drug loading microspheres. Hyaluronic acid (HA) and polylysine (Pls) were used as internal phase additives to see their influences on the drug loading and releasing. Double emulsion (water-in-oil-in-water) solvent extraction/evaporation method was used for the purpose. Particle size analysis display that the polyelectrolytes have low impact on the microsphere average size and distribution. Scanning electron microscope (SEM) pictures show the wrinkled surface resulted by the internal microcavity of the microspheres. Microspheres with HA inside have higher drug loading amounts than microspheres with Pls inside. The loading drug amounts of the microspheres increase with the HA amounts inside, while decreasing with the Pls amounts inside. All the polyelectrolytes adding groups have burst release observed in experiments. The microspheres with Pls internal phase have faster release rate than the HA groups. Among the same polyelectrolyte internal phase groups, the release rate increases with the amounts increasing when Pls is inside, while it decreases with the amounts increasing when HA is inside.
    Full-text · Article · Feb 2014
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    • "Although some studies report low entrapment efficiency (EE) [3], the double emulsion (water-in-oil-inwater , W 1 /O/W 2 ) solvent evaporation is an advantageous technique because it provides higher protection for the substance to be encapsulated. Nevertheless, it is possible to increase the encapsulation capability of the system by modifying the double emulsion preparation conditions [7] [9] [2] [1]. Also, Errico et al. [5] recently reported a new technique for PHB drug-loaded capsules via dialysis. "
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    ABSTRACT: Natural and synthetic biodegradable polymers have been investigated for controlled drug release. Poly(3-hydroxybutyrate) can be produced by bacteria and is remarkable for this application due to its excellent biocompatibility and biodegradability. The objective of this work was to study different drug-entrapment and emulsification methods for the obtaining of doxycycline-loaded PHB micro- and nano-spheres. The micro-/nano-particles were prepared by polymer precipitation via dialysis, simple emulsion (O/W) or multiple emulsion (W-1/O/W-2) applying solvent evaporation in the last two cases. This was carried out either by ultrasonication, dripping and/or high speed stirring. Different processing conditions were varied in order to evaluate their influence on morphology, size, and drug entrapment capabilities. The highest drug loading was obtained by single emulsion with high speed stirring. In the case of multiple emulsion, the combination of ultrasound with high speed stirring resulted in the most elevate process yield and drug loading capability.
    Full-text · Article · Aug 2013 · European Polymer Journal
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    • "Although some studies report low entrapment efficiency (EE) [3], the double emulsion (water-in-oil-inwater , W 1 /O/W 2 ) solvent evaporation is an advantageous technique because it provides higher protection for the substance to be encapsulated. Nevertheless, it is possible to increase the encapsulation capability of the system by modifying the double emulsion preparation conditions [7] [9] [2] [1]. Also, Errico et al. [5] recently reported a new technique for PHB drug-loaded capsules via dialysis. "
    [Show abstract] [Hide abstract]
    ABSTRACT: Natural and synthetic biodegradable polymers have been investigated for controlled drug release. Poly(3-hydroxybutyrate) can be produced by bacteria and is remarkable for this application due to its excellent biocompatibility and biodegradability. The objective of this work was to study different drug-entrapment and emulsification methods for the obtaining of doxycycline-loaded PHB micro- and nano-spheres. The micro-/nano-particles were prepared by polymer precipitation via dialysis, simple emulsion (O/W) or multiple emulsion (W1/O/W2) applying solvent evaporation in the last two cases. This was carried out either by ultrasonication, dripping and/or high speed stirring. Different processing conditions were varied in order to evaluate their influence on morphology, size, and drug entrapment capabilities. The highest drug loading was obtained by single emulsion with high speed stirring. In the case of multiple emulsion, the combination of ultrasound with high speed stirring resulted in the most elevate process yield and drug loading capability.
    Full-text · Article · Aug 2013 · European Polymer Journal
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