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Glyceryl Tristearate/Tristearin

Tristearin or glyceryl tristearate is an odourless, white powder. It is a triglyceride derived from three units of stearic acid. Most triglycerides are derived from at least two and more commonly three different fatty acids. Like other triglycerides, stearin can crystallise in three polymorphs.

Skeletal formula of tristearin.Fig.1 Skeletal formula of tristearin.

Tristearin has been used in the development of drug delivery carriers. Matrix systems prepared using triglycerides have been shown to protect labile or altered agents from degradation and allow controlled drug release. Specifically, tristearin has been utilized to demonstrate efficient immobilisation of drugs through high-pressure homogenisation which suggests the material is viable and applicable to more aggressive processing routes (e.g. when compared to emulsion methods). Tristearin-based drug delivery systems are valuable in the development of drug carriers for improving their bioavailability by better diffusion through biological membranes.

Nanostructured Lipid Carrier Based on Tristearin/Tricaprin Mixture as Delivery Systems for Bromocriptine

Nanoparticles based on solid lipids (SLN) such as triglycerides have been proposed as novel drug carrier systems. Due to the lipophilic nature of their matrix, solid triglyceride nanoparticles are considered particularly useful for the administration of lipophilic drugs. SLN based on different lipidic components has been produced and characterized. Bromocriptine (BK) was encapsulated with the highest entrapment efficiency in a tristearin/tricaprin mixture able to guarantee long-term stability and prolonged drug release. The encouraging results suggest that NLC based on tristearin/tricaprin mixture could be proposed as an innovative system to administer BK during PD therapy. This system may represent a novel strategy to achieve stable drug levels thereby increasing patients’ compliance to the therapy and reducing long-term side effects.

Cryo-transmission electron microscopy images (cryo-TEM) of SLN dispersions constituted of tristearin (A), tristearin-monostearin (2:1) (B), tristearin-tricaprin (2:1) (C), tribehenin (D) and tristearin-tricaprin (2:1).Fig.2 Cryo-transmission electron microscopy images (cryo-TEM) of SLN dispersions constituted of tristearin (A), tristearin-monostearin (2:1) (B), tristearin-tricaprin (2:1) (C), tribehenin (D), and tristearin-tricaprin (2:1). (Esposito, 2008)

Lipid Nanocarrier with Tristearin for Ocular Delivery of Hydrophilic Drug

Lipid nanocarrier (like solid lipid nanoparticle) possesses good biocompatibility, low toxicity, and high drug loading attributes in contrast to the polymeric carrier, which makes it an obvious choice for ophthalmic drug delivery. Stearic acid and tristearin were selected as the lipid carrier while Poloxamer 188 and sodium taurocholate was used as surfactant and co-surfactant, respectively. Solid lipid nanoparticles (SLNs) were then evaluated for improved ocular delivery of Valacyclovir (VAC). The submicron size, good stability, acceptable pH range, higher entrapment efficiency, and ameliorated corneal permeation fulfill the prerequisites for an optimized ocular formulation, demonstrating the potential of lipid nanocarriers in the efficient ocular delivery of hydrophilic molecules.

TEM images of VAC SLNs.Fig.3 TEM images of VAC SLNs. (Kumar, 2017)

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References

  1. Esposito. E.; et al. Solid lipid nanoparticles as delivery systems for bromocriptine. Pharmaceutical research. 2008, 25(7): 1521-1530.
  2. Kumar, R.; Sinha, V.R. Lipid nanocarrier: an efficient approach towards ocular delivery of hydrophilic drug (Valacyclovir). AAPS PharmSciTech. 2017, 18(3): 884-894.
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