Semi-Phyto Universal Solubilizer (SPUS) for enhancing solubility and bio availability of Bioactive compounds

Aqueous Solubility of Bio actives plays a significant role in Drug, Biopharma, Food, Dietary and Cosmetic formulations. Poor solubility is one of the biggest hurdles in developing these formulations as well as desired therapeutic effect. It is well proven that more aqueous soluble means rapid absorption which leads to more bioavailability in the body thereby decreases the dosage of Actives to a greater extent.

In food specifically, the beverage industry suffers a lot with unavailability of Natural solubilizer. Moreover, the Cosmetic industry couldn’t use some of the Phyto actives in their formulations due to non-aqueous solubility, even though they possess excellent biological activity.

What is Aqua-D?

Aqua-D is Semi-Phyto Universal Solubilizer (SPUS) and scientifically known as Diosgenin Polyethylene glycol succinate) is a water-soluble form of naturally occurring Diosgenin. Diosgenin, a steroidal sapogenin, occurs abundantly in plants such as Dioscorea alata, Smilax China, and Trigonella foenum graecum. This bioactive phytochemical not only is used as an important starting material for the preparation of several steroidal drugs in the pharmaceutical industry but has revealed also high potential and interest in the treatment of various types of disorders such as cancer, hypercholesterolemia, inflammation, and several types of infections. In fact, diosgenin has been described in the literature for its pharmacological potential, including the interesting underlying mechanisms of action, thereby confirming and extending the knowledge from its usage in traditional medicine. In this context, mainly over the past two decades, a series of preclinical and mechanistic studies have been performed to understand the real importance and benefits of diosgenin against a variety of pathologies including metabolic diseases (diabetes, obesity, and dyslipidemia, including hypercholesterolemia), inflammatory diseases, and cancer.
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Aqua-D is produced by the esterification of Diosgenin succinate by polyethylene glycol 1000. In addition to serving as a water-soluble source of Diosgenin, AquaD-is an amphiphilic compound with hydrophilic head and Lipophilic Tail. This dual combination of lipophilic and hydrophilic activities in a single molecule imparts unique properties. Aqua-D is a unique water soluble natural Diosgenin, used to enhance the bioavailability of Bio actives. It is a powerful emulsifier and solubilizer for fat soluble ingredients, as well as ingredients with poor solubility. Aqua-D is a miscible form of Diosgenin, is composed of a hydrophobic Diosgenin part and a hydrophilic PEG chain. It exhibits excellent drug delivery capability based on this special amphiphilic structure.

Solubility enhancement
Curcumin, from the spice turmeric, exhibits anti-inflammatory, antioxidant, anticancer, antiviral and neurotrophic activity and therefore holds promise as a therapeutic agent to prevent and treat several disorders. However, a major barrier to curcumin’s clinical efficacy is its poor bioavailability. Efforts have therefore been dedicated to developing curcumin formulations with greater bioavailability and systemic tissue distribution.
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Solubilizing capacity of AquaD-1000
Curcumin is formulated with Aqua-D Hot-melt process.

Enhancing Bioavailability-Comparison of Release profile
Curcumin, a major active constituent found in Curcuma sp, is classified in group 4 of BCS (Biopharmaceutical Class System). This means solubility is a key factor when determining the absorption. In addition, low permeability is a second contribution for its low bioavailability after oral administration. According to Banrida et al., tested curcumin in CaCo2 cells indicated that curcumin is poorly permeable with a Papp (A → B) value of 2.93 ± 0.94 106 cm/s. Papp value in (B → A) study was found out to be 2.55 ± 0.02 106 cm/s, thus ruling out the role of efflux pathways in the low oral bioavailability of curcumin. In addition to poor solubility and permeability, the low bioavailability of curcumin is also worsened by intensive hepatic metabolism to more hydrophilic substances which are inactive.  In relation to that study, we also did an in vitro assay of challenging curcumin in liver homogenate and observed rapid degradation after incubation at 37 °C. Curcumin is reported as a potent anti-inflammatory agent; however, its complex problems led to clinical failure when this compound was used. BCS 4 drugs like curcumin are difficult to solve especially in the phase of formulation and delivery.

Interested to learn more? Download the full whitepaper here: White paper AquaD_PHARMAEXCIPIENTS

Whitepaper written by Velmurugan Shanmugham

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