Abstract

The absorption, distribution, biotransformation and excretion of a drug involve its transport across cell membranes. This process is essential and influenced by the characteristics of the drug, especially its molecular size and shape, solubility at the site of its absorption, relative lipid solubility, etc. One of the progressive ways for increasing bioavaibility is a nanoparticle preparation technique. Cholesterol, cholestenolone and pregnenolone acetate as model active pharmaceutical ingredients and some of the commonly used excipients as nanoparticle stabilizers were used in the investigated precipitation method that was modified and simplified and can be used as an effective and an affordable technique for the preparation of nanoparticles. All 120 prepared samples were analyzed by means of dynamic light scattering (Nanophox). The range of the particle size of the determined 100 nanoparticle samples was from 1 nm to 773 nm, whereas 82 samples contained nanoparticles of less than 200 nm. Relationships between solvents and used excipients and their amount are discussed.

Highlights

  • For achieve the pharmacological activity of an active pharmaceutical ingredient (API), the solubility of the API in physiological liquids is required, so that the API can be available at the place of absorption

  • Sodium dodecyl sulfate (SDS, sodium lauryl sulfate) is an anionic surfactant consisting of a C12 tail attached to a sulfate group, giving the compound the desired amphiphilic properties

  • It is often used as salt-sodium carboxymethyl cellulose (SCMC)

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Summary

Introduction

For achieve the pharmacological activity of an active pharmaceutical ingredient (API), the solubility of the API in physiological liquids is required, so that the API can be available at the place of absorption. The solubility of a compound in water correlates to a great extent with the solubility in physiological liquids and is the first limiting factor for good absorption and biodistribution. From the point of view of pharmaceutical formulations, the solubility of compounds higher than 1% can be considered as satisfactory. When this condition is not met, it is important to improve the solubility. Solubility is not the only important factor; the solubility rate is essential. This is a physico-chemical property that can be influenced by crystal shape (morphology, polymorphism), particle size, properties of compound surface, etc. This is a physico-chemical property that can be influenced by crystal shape (morphology, polymorphism), particle size, properties of compound surface, etc. [1,2,3]

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