Abstract
Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic anticancer drugs) based on effectiveness and safety profile. Biologic drugs are administered by intravenous (IV) injection due to their large molecular weight, while small molecule drugs are preferentially administered by gastrointestinal route. Even though IV injection is the fastest route of administration and ensures complete bioavailability, this route of administration causes patient inconvenience to visit a hospital for anticancer treatments. In addition, IV administration can cause several side effects such as severe hypersensitivity, myelosuppression, neutropenia, and neurotoxicity. Oral administration is the preferred route for drug delivery due to several advantages such as low cost, pain avoidance, and safety. The main problem of NCEs is a limited aqueous solubility, resulting in poor absorption and low bioavailability. Therefore, improving oral bioavailability of poorly water-soluble drugs is a great challenge in the development of pharmaceutical dosage forms. Several methods such as solid dispersion, complexation, lipid-based systems, micronization, nanonization, and co-crystals were developed to improve the solubility of hydrophobic drugs. Recently, solid dispersion is one of the most widely used and successful techniques in formulation development. This review mainly discusses classification, methods for preparation of solid dispersions, and use of solid dispersion for improving solubility of poorly soluble anticancer drugs.
Highlights
Cancer is one of the leading causes of death worldwide, and treatment remains a great challenge
We focused on classification of solid dispersion (SD), methods for preparation of SD, and current trends in SD for improving the solubility of poorly water-soluble drugs, including anticancer drugs
Patients are inconvenienced by this route because they have to visit a hospital to receive treatment
Summary
Cancer is one of the leading causes of death worldwide, and treatment remains a great challenge. Vinothini et al [5] developed a graphene oxide-methyl acrylate-FA/paclitaxel (GO-MA-FA/PTX) nanocarrier for targeted anticancer drug delivery to breast cancer cells, resulting in reduction of 39% of typical cytotoxic effects. Development of nanoparticle anticancer drugs has improved therapeutic efficacy because the drug can be directly and selectively targeted to cancer cells [8,9,10]. To improve the solubility and BA of poorly water-soluble drugs, several methods have been developed such as solid dispersion (SD) [23,24,25], complexation [26], lipid-based systems [27,28], micronization [29,30], nanonization [31,32,33], and co-crystals [34,35]. SD is defined as a group of solid products consisting of a hydrophobic drug dispersed in at least one hydrophilic carrier, resulting in enhanced surface area, leading to higher drug solubility and dissolution rate. ManyMcaanryricearrsriaerrseaurseeudseidn iSnDS.DT. hTehseeseccaarrrriieerrss ddeetteerrmmiinneeththeefifinanlaflofromrumlautiloantiopnroppreortpieesratineds caannd can be catbeegcoartiezgeodrizinetdoinfitrostf,irsset,csoencdon, da,nadndthtihridrdclcalassseess((FFiiguree 22))
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