Abstract
Hot-melt granulation is a technique used to obtain granules by dispersing a drug in polymers at a high temperature. Tenofovir, an antiretroviral drug with proven activity as a vaginal microbicide, was dispersed in melted Gelucire® (or a mixture of different Gelucire®) to obtain drug-loaded granules. Studies performed on the granules proved that the drug is not altered in the hot-melt granulation process. The granules obtained were included in a matrix formed by the hydrophilic polymers hydroxypropylmethylcellulose and chitosan to obtain vaginal tablets that combine different mechanisms of controlled release: The Gelucire® needs to soften to allow the release of the Tenofovir, and the hydrophilic polymers must form a gel so the drug can diffuse through it. The studies performed with the tablets were swelling behavior, Tenofovir release, and ex vivo mucoadhesion. The tablets containing granules obtained with Tenofovir and Gelucire® 43/01 in a ratio of 1:2 in a matrix formed by hydroxypropylmethylcellulose and chitosan in a ratio of 1.9:1 were selected as the optimal formulation, since they release Tenofovir in a sustained manner over 216h and remain attached to the vaginal mucosa throughout. A weekly administration of these tablets would therefore offer women protection against the sexual transmission of HIV.
Highlights
IntroductionThe most common applications of this technique in pharmaceutical development are targeted drug release, masking the taste of active substances, and improving the solubility of poorly soluble drugs [3]
The hot-melt granulation technique consists of dissolving or dispersing an active principle in one or more melted polymers in order, after cooling, to obtain granules with a defined structure [1].The melt entropy of the different components determines whether they will crystallize simultaneously, in turn conditioning the microstructure of the granules in the solid state [2].The most common applications of this technique in pharmaceutical development are targeted drug release, masking the taste of active substances, and improving the solubility of poorly soluble drugs [3]
Solid dispersions of the drug are usually prepared in an inert hydrophilic matrix, causing the active principle to convert from its crystalline state to an amorphous form and improving its solubility [4]
Summary
The most common applications of this technique in pharmaceutical development are targeted drug release, masking the taste of active substances, and improving the solubility of poorly soluble drugs [3] In the latter case, solid dispersions of the drug are usually prepared in an inert hydrophilic matrix, causing the active principle to convert from its crystalline state to an amorphous form and improving its solubility [4]. Solid dispersions of the drug are usually prepared in an inert hydrophilic matrix, causing the active principle to convert from its crystalline state to an amorphous form and improving its solubility [4] This technique could be applied in reverse to delay the dissolution of water-soluble drugs, which would aid the development of sustained-release systems capable of releasing the drug at a given rate, thereby achieving a constant concentration of the active principle at the site of action [3,4]. Another advantage is that Gelucire® is commercialized with different melting points and hydrophilic-lipophilic balances (HLB), offering a wide range of options from which to select the most suitable for our purposes [11]
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