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Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content

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Abstract

Purpose

Aim was to formulate oil-in-water (O/W) microemulsion with a high volume ratio of complex natural oil, i.e. copaiba oil and low surfactant content. The strategy of formulation was based on (i) the selection of surfactants based on predictive calculations of chemical compatibility between their hydrophobic moiety and oil components and (ii) matching the HLB of the surfactants with the required HLB of the oil.

Method

Solubility parameters of the hydrophobic moiety of the surfactants and of the main components found in the oil were calculated and compared. In turn, required HLB of oils were calculated. Selection of surfactants was achieved matching their solubility parameters with those of oil components. Blends of surfactants were prepared with HLB matching the required HLB of the oils. Oil:water mixtures (15:85 and 25:75) were the titrated with surfactant blends until a microemulsion was formed.

Results

Two surfactant blends were identified from the predictive calculation approach. Microemulsions containing up to 19.6% and 13.7% of selected surfactant blends were obtained.

Conclusion

O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.

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Abbreviations

Ehi :

Hydrogen bonding energy of the partial group

Fdi :

Dispersion energy of the partial group

Fpi :

Polar energy of the partial group

GC-FID:

Gas chromatography – flame ionization detector

GC-MS:

Gas chromatography–mass spectrometry

HLB:

Hydrophilic-lipophilic balance

HLB0 :

Required hydrophilic-lipophilic balance

HLB0essential oil :

Required hydrophilic-lipophilic balance of copaiba essential oil

HLB0oil :

Required hydrophilic-lipophilic balance of an oil

HLB0resin :

Required hydrophilic-lipophilic balance of copaiba resin oil

K:

Constant applied to O/W emulsion

O/W:

Oil-in-water

PdI:

Polydispersity index

V:

Molar volume

W:

Weight fractions of the surfactants/ compound

δd :

Dispersive partial solubility parameters

δh :

Hydrogen bonding partial solubility parameters

δp :

Polar partial solubility parameters

δt :

Total solubility parameter

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ACKNOWLEDGMENTS AND DISCLOSURES

This work was financially supported by the “coordenação de aperfeiçoamento de pessoal de nível superior” CAPES COFECUB 721/11. The authors wish to thank Dr Alexandre Maciuk for his help in the dosage of Copaiba Oil.

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Authors and Affiliations

  1. Université Paris-Sud, Institut Galien Paris Sud - UMR CNRS 8612 - Faculté de Pharmacie, 92296, Chatenay-Malabry Cedex, France

    Francisco Humberto Xavier-Junior, Nicolas Huang, Jean-Jacques Vachon & Christine Vauthier

  2. Universidade Federal do Rio Grande do Norte, Centro de Ciências da Saúde, Departamento de Farmácia, Laboratório de Sistemas Dispersos (LaSiD), Av. Gal. Gustavo Cordeiro de Farias, S/N, Petrópolis, 59010-180, Natal, RN, Brazil

    Francisco Humberto Xavier-Junior & Eryvaldo Sócrates Tabosa do Egito

  3. Universidade Estadual de Campinas (UNICAMP) – Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas. Rua Alexandre Cazelatto, 999, Vila Betel, Paulínia, SP, Brazil

    Vera Lucia Garcia Rehder

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  1. Francisco Humberto Xavier-Junior
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  2. Nicolas Huang
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Correspondence to Christine Vauthier.

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Xavier-Junior, F.H., Huang, N., Vachon, JJ. et al. Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content. Pharm Res 33, 3031–3043 (2016). https://doi.org/10.1007/s11095-016-2025-y

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