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.

Benign prostatic hyperplasia (BPH) is the most common condition in elderly men that is characterized by an increase in the size of the prostate gland. Cinnamomum cassia and Rosa laevigata have been reported to treat the symptoms associated with BPH. The aim of this study was to evaluate the effects of HT080, an herbal extract of C. cassia and R. laevigata, on a testosterone propionate (TP)-induced BPH rat model. The rats received a daily subcutaneous injection of TP (3 mg/kg) for 4 weeks to induce BPH. Rats were divided into four groups: group 1 (sham), group 2 (BPH, TP alone), group 3 (Fina, TP + finasteride 1 mg/kg/day), and group 4 (HT080, TP + HT080 200 mg/kg/day). At the end of the experiment, all rats were sacrificed, and their prostate glands were removed, weighed, and subjected to histopathological examination and western blot analyses. Serum testosterone and dihydrotestosterone (DHT) levels were determined. In addition, serum alanine and aspartate aminotransferase levels were measured to evaluate the toxicity in the liver. The Hershberger bioassay was also conducted to investigate the effects of HT080 on androgenic and antiandrogenic activities. In the BPH model, the prostate weight, prostate index, prostate epithelial thickness, and serum testosterone and DHT levels in the HT080 group were significantly reduced compared to the BPH group. Histological studies showed that HT080 reduced prostatic hyperplasia. The protein expression of androgen receptor from the HT080 group was significantly reduced in comparison with the BPH group (p < 0.05). HT080 also induced apoptosis by regulating Bcl-2 and Bax expression. In addition, HT080 showed no toxicity in the liver and did not exhibit androgenic and antiandrogenic activities. Our finding revealed that HT080 can be a potential candidate for the treatment of BPH by regulating androgen receptor signaling and apoptosis.

Background/Objectives: Benign prostatic hyperplasia (BPH) is prevalent among older men and is often accompanied by lower urinary tract symptoms (LUTS), including storage and voiding symptoms. Achyranthis Radix, the root of Achyranthes bidentata, is commonly used as a functional food in Asia and has been documented in traditional medicine for conditions associated with LUTS. However, its effects on BPH have not been experimentally investigated. Therefore, this study evaluated an ethanolic extract of Achyranthis Radix (ARE) in a rat model of testosterone propionate (TP)-induced BPH. Methods: Male Sprague-Dawley rats were randomly assigned to six groups: sham, control, finasteride (1 mg/kg), and ARE (30, 100, or 300 mg/kg). BPH was induced in all groups except the sham group by castration followed by subcutaneous administration of TP (3 mg/kg/day) for 4 weeks. ARE and finasteride were orally administered once daily concurrently with TP treatment. Prostate weight, prostate index, histological changes, serum androgen levels, androgen receptor (AR) expression, and apoptosis-related proteins were evaluated. Results: ARE significantly reduced prostate weight and prostate index and attenuated BPH-associated histological changes compared with the control group. ARE also significantly decreased serum dihydrotestosterone levels and reduced prostatic AR expression. In addition, ARE modulated the expression of apoptosis-related proteins in the prostate. Conclusions: ARE attenuated the development of prostate enlargement in rats when administered concurrently with TP. The accompanying changes in serum androgen levels and prostatic androgen-related and apoptosis-related protein expression provide a basis for further mechanistic investigation. These findings support further evaluation of ARE for BPH management.