Liquisolid technique and its applications in pharmaceutics

Most of the newly developed drug candidates are lipophilic and poorly water-soluble. Enhancing the dissolution and bioavailability of these drugs is a major challenge for the pharmaceutical industry. Liquisolid technique, which is based on the conversion of the drug in liquid state into an apparently dry, non-adherent, free flowing and compressible powder, is a novel and advanced approach to tackle the issue. The objective of this article is to present an overview of liquisolid technique and summarize the progress of its applications in pharmaceutics. Low cost, simple processing and great potentials in industrial production are main advantages of this approach. In addition to the enhancement of dissolution rate of poorly water-soluble drugs, this technique is also a fairly new technique to effectively retard drug release. Furthermore, liquisolid technique has been investigated as a tool to minimize the effect of pH variation on drug release and as a promising alternative to conventional coating for the improvement of drug photostability in solid dosage forms. Overall, liquisolid technique is a newly developed and promising tool for enhancing drug dissolution and sustaining drug release, and its potential applications in pharmaceutics are still being broadened

The effects of PPARγ inhibitor on bones and bone marrow fat in aged glucocorticoid-treated female rats

Progressive bone marrow (BM) fat accumulation is a common bone loss characteristic in older populations and glucocorticoid (GC)-induced skeletal destruction that is inversely associated with bone synthesis and directly associated with increased peroxisomal proliferator-activated receptor gamma (PPARγ) expression. PPARγ inhibition is an efficient therapeutic strategy for aged- and GC-related skeletal disorders. This study aimed to evaluate the effect of PPARγ inhibition on aged GC-treated female rats. It was hypothesised that bisphenol A diglycidyl ether (BADGE) could inhibit marrow adiposity and improve osteogenesis by inhibiting PPARγ, thereby preventing GC-induced osteoporosis (GIO). Female Sprague–Dawley rats (n = 32, age = 18 months) were randomly allocated to one of the following groups: (1) control, (2) BADGE (30 mg/kg/day, intraperitoneal), (3) methylprednisolone (MP; 30 mg/kg/day, subcutaneous), and (4) MP + BADGE. After eight weeks of treatment, bone density (BD) and trabecular bone microarchitectures were quantified by micro-computed tomography (CT), and BM adipocytes were quantified by histopathology. Additionally, mRNA and protein expression of adipogenic and osteogenic markers were quantified by reverse transcription-quantitative polymerase chain reaction. Furthermore, serum bone turnover biomarker levels were quantified by enzyme-linked immunosorbent assay. MP treatment led to marrow adipogenesis and bone deterioration. However, rats treated with MP + BADGE showed lower marrow adipogenesis, as indicated by smaller marrow adipocyte diameter, decreased density and area percentages, reduced expression of marrow adipogenic genes and proteins, improved BD and trabecular microarchitectures, increased expression of osteogenic genes and proteins, and higher levels of serum bone formation markers. These results were consistent with the differences observed between control and BADGE mono-treated rats. In conclusion, BADGE treatment attenuates BM adiposity and improves bone formation in aged GC-treated female rats by inhibiting PPARγ. Therefore, PPARγ might be a potential target for treating GIO in older populations

Guanidinoacetic Acid Supplementation Promotes Skeletal Muscle Fiber Type Transformation from Fast-to-Slow-Twitch via Increasing the PPARGC1A Based Mitochondrial Function and CaN/NFAT Pathway in Finishing Pigs

Guanidinoacetic acid can improve pork quality. Previous studies have demonstrated that pork quality is closely linked to the muscle fiber type mediated by PPARGC1A. Therefore, this study aimed to evaluate the influence of dietary GAA supplementation on the skeletal muscle fiber type transformation. A total of 180 healthy Duroc × Landrace × Meishan cross castrated male pigs with a similar average weight (90 ± 1.5 kg) were randomly divided into three treatments with five replicates per treatment and 12 pigs per replicate, including a GAA-free basal diet and basal diet with 0.05% or 0.10% GAA for 15 days. Our results showed that 0.10% GAA supplementation increased the contents of Ca2+ in sarcoplasm (p p p p p p < 0.05). Overall, dietary GAA supplementation promotes skeletal muscle fiber types transformation from fast-to-slow-twitch via increasing the PPARGC1A based mitochondrial function and the activation of CaN/NFAT pathway in finishing pigs