Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

Osteoporosis (OP) is considered as one of the major comorbidities of rheumatoid arthritis (RA), and is responsible for fragility fracture. However, there is currently no effective treatment for RA complicated with OP. Tubson-2 decoction (TBD), a Mongolian medicine also known as Erwei Duzhong Decoction, has been shown to exert a preventive effect on post-menopausal osteoporosis (PMOP). The preventive effects of TBD on RA-induced OP, as well as the bioactive compound responsible and the underlying mechanisms, remain to be elucidated. To explore the effects of TBD on RA-induced OP in vivo, and to elucidate the mechanism of isochlorogenic acid A (ICA), the effective component of TBD, in vitro. To evaluate the anti-arthritic and anti-osteoporotic effects of TBD, we conducted H&E straining and safranine O/fast green, TEM, immunohistochemistry (IHC), bone histomorphometry, micro-CT imaging, and biomechanical testing in collagen induced arthritis (CIA) rats. The active ingredient in TBD was identified using network pharmacology and molecular docking. The identification was supported by in vivo IHC assay, and further confirmed using qRT-PCR, Western blot, and SEM analysis in TNF-α-treated MH7A cells and/or in LPS-exposed RAW264.7 cells. Oral administration of TBD attenuated the severity of arthritis and osteopenia as well as poor bone quality, in CIA rats. Additionally, TBD and the positive control, tripterygium glycosides (TG), exhibited similar effects in reducing inflammation in both the synovium and ankle joint. They also were both effective in improving bone loss, microarchitecture, and overall bone quality. TBD reduced the expression of MMP13, IL-17, and p-JNK protein in the synovium of CIA rats. ICA, which was screened, suppressed TNF-α or LPS-triggered inflammatory responses via down-regulating IL-17 signaling, involving in MMP13, IL-1β, IL-23, and IL-17, and the MAPK pathway including p-ERK, p-JNK, and p-P38, both in MH7A cells and in RAW264.7 cells. Furthermore, ICA prevented osteoclasts from differentiating and bone resoprtion in a dose-dependent manner in vitro. This study provides the first evidence that TBD exerts intervening effects on RA-induced OP, possibly through the downregulation of the IL-17/MAPK signaling pathway by ICA. The findings of our study provides valuable insights for further research in this area.

Daodi medicinal materials (DMMs), with unique characteristics and specific ecological growing environments, are recognized as high-quality medicinal products of Chinese medicinal materials (CMMs). The quality evaluation of CMMs is fundamental for standardization. The concept and application of DMMs have a long history as described in records in ancient books and rooted in practice and experience over generations. DMM is the specific term for pure, superior medicinal herbs with the following characteristics: optimum harvest season (reflecting the appropriate developmental stage of the plant), scrupulous processing, traditional preparation technology, etc. As DMM and high-quality medicinal products are traditionally thought to be closely related, modern scientific studies that confirm the association of these products are described. This article aims to clarify the scientific elucidation of DMMs.

Traditional Chinese Medicine (TCM) usually contains one specific class of components that could represent its phytochemical properties and therapeutic effects. However, the unclear specific class constituents hinders the sufficient interpretation of its bioactivities. In this paper, an HPLC-LTQ-Orbitrap-based strategy focused on the TCM targeted class was developed. This strategy was successfully applied in the discovery and identification of phenylethanoid glycosides (PhGs) in Herba Cistanches, and herbomics research of Cistanche deserticola, C. sinensis, and C. tubulosa. A total of 69 PhGs, including 17 new PhGs, were rapidly discovered and characterized using multiple data-mining methods such as accurate parent mass search, parent mass modification search and fragment ion search, allowing a comprehensive revelation of PhGs in Cistanche species for the first time. Based on the peak areas of the 69 PhGs identified, multivariate statistical analysis such as PCA, loading analysis and OPLS-DA were employed in herbomics research to screen and validate the PhGs that could be utilized to discriminate these three Cistanche species. Eight PhGs were finally screened and chosen as chemical markers for the species discrimination. In conclusion, this new established strategy could be exemplary for future studies on the discovery and identification of important chemical constituents, and differentiation of genuine specie or genus from adulterants. Meanwhile, it may propose a novel idea for analyzing a specific class of active chemical constituents, and is promising for quality control and evaluation of TCMs.