Preparation of a solid-in-oil nanosuspension containing l-ascorbic acid as a novel long-term stable topical formulation

l-Ascorbic acid (AA, vitamin C) easily decomposes into inactive compounds in aqueous solutions and this has limited its topical use. This work reports the preparation of a solid-in-oil nanosuspension (SONS) containing AA and validation of its basic storage stability. Although AA itself is water-soluble, it can readily be nanosuspended in squalane via complex formation involving a combination of sucrose erucate (i.e. lipophilic surfactant) and sucrose monolaureate (i.e. hydrophilic surfactant) to yield SONS with a very low moisture content (<500 ppm). To extract encapsulated AA, a lipase-based enzymatic degradation technique was used to degrade a formulation phase making it easier for AA to distribute into an extraction solution. Our results demonstrate that almost all the encapsulated AA (95.3%) was readily extracted from the SONS upon addition of medium-chain triglyceride, which offers the possibility of degrading the formulation phase using lipase. Finally, its storage stability study was investigated at 25 °C over 90 days under protection from light. An aqueous solution containing AA was used as a control. Compared with the control, the SONS markedly increased the stability of AA due to its low moisture content and, thus, the potential usefulness SONSs as a novel long-term stable topical formulation of AA has been proved.

Graphical abstractl-Ascorbic acid (AA, vitamin C) easily decomposes into inactive compounds in aqueous solutions and this has limited its topical use. This work reports the preparation of a solid-in-oil nanosuspension (SONS) containing AA and validation of its basic storage stability. Although AA itself is water-soluble, it can readily be nanosuspended in squalane via complex formation involving a combination of sucrose erucate (i.e. lipophilic surfactant) and sucrose monolaureate (i.e. hydrophilic surfactant) to yield SONS with a very low moisture content (<500 ppm). The results obtained demonstrated that the SONS markedly increased the stability of AA due to its low moisture content.Figure optionsDownload full-size imageDownload as PowerPoint slide