Determination of the bioavailability and biodistribution of a single dose of oral cholecalciferol/Calcirol® soft gelatin capsule by pharmacoscintigraphy- CalSci study

Background: It is required to study the bioavailability and biodistribution of specific cholecalciferol formulation before prescribing. Pharmacoscintigraphy is an established radiological-imaging technique that is used to map various drug formulations as they traverses the human body (biodistribution) in real-time. We evaluated the bioavailability and biodistribution pattern, transit time, and gastrointestinal clearance of a single dose of Calcirol® soft gelatin capsule 60,000 IU [an oral cholecalciferol (vitamin D) formulation] using pharmacoscintigraphy. Methods: Six male healthy adult volunteers were administered a single oral dose of Calcirol® soft gelatin capsule labelled with technetium-99m. Post-dosing, serial venous blood samples were collected till day 27 for the estimation of the plasma levels of 25-hydroxycholecalciferol and 1,25-dihydroxycholecalciferol levels. Different pharmacokinetic parameters were calculated. Sequential static gamma imaging was performed to evaluate the biodistribution of Calcirol® soft gelatin capsule. Descriptive statistics was used. Various pharmacokinetic parameters were calculated from the concentration-time curves. Statistical analysis was carried out using Student’s t-test. Suitable multivariate analysis was performed based on the distribution of data. All statistical analyses were performed using SAS® Software (v 9.4). Results: The overall absorption of Calcirol® soft gelatin capsule was 93.23%, which was fully from the small intestine. It led to achieving a sufficient level of 25-hydroxycholecalciferol (>60 ng/ml) within 6 hours of oral intake. The levels of plasma 25-hydroxycholecalciferol and 1,25-dihydroxycholecalciferol increased (maximum around 6 and 18 days, respectively). The small intestinal residence time was around 16 hours. No adverse event was noted. Conclusions: This was the first pharmacoscintigraphy study in the world which demonstrated the favourable bio-distribution of the Calcirol softgels supporting its role in vitamin D supplementation

In vivo-wound healing studies of sodium thiosulfate gel in rats

Sodium Thiosulfate (STS) is already reported as an antioxidant, anti-inflammatory agent with antiseptic, antifungal properties. The search for an ideal antiseptic still continues, which is lethal to all types of bacteria and their spores and sustain the activity for a longer time without any harm to the host tissue. The aim of the present study is to evaluate the effect of STS on curing of wounds in rats when compared to Betadine. We developed topical gels having 6% and 12% STS. The effects of STS on wound healing rate of Rats were evaluated against Betadine as positive control. Wounds of control group, selected as Group 1 was treated with normal saline (0.2 ml), twice a day. Reference standard control, designated as Group 2 rats were given with 0.2 ml Betadine twice a day. Rats in Groups 3 and 4 were treated with 0.2 ml of STS gel (6% or 12% respectively) twice a day. In our study, STS formulation has proved to be a safe and efficient wound healing product. It has a neutral pH and longer half life (>12 months). Higher STS dose of 12% proved to have a wound curing rate equivalent to that of Betadine. On 11th Day, 97 ± 0.79% healing was achieved with Betadine and 98 ± 0.67% with 12% STS Gel (∗P < 0.05). Microscopic images of H&E stained skin tissue from animals treated with Betadine and 12% STS formulation showed a reduction in scar size, lesser amount of inflammatory cells, higher fibroblasts and blood vessels, with considerable collagen accumulation. Furthermore, a significant enhancement in the levels of GPx, CAT and SOD was observed in the tissue at the wound site of the treated group. The IL 10 levels in both groups of STS-treated rats was increased, whereas, TNF-α levels were reduced significantly in tissue homogenate compared with control. Thus, this study shows the wound-healing performance of STS formulation. Further studies are necessary to understand the real mechanism of how STS formulation heals wounds

Colon cancer and their targeting approaches through nanocarriers: A review

Colon cancer is the fifth most common type of cancer in the world. Colon cancer develops when healthy cells in the lining of the colon or rectum alter and grow uncontrollably to form a mass known as a tumor. Despite major medical improvements, colon cancer is still one of the leading causes of cancer-related mortality globally. One of the main issues of chemotherapy is toxicity related to conventional medicines. The targeted delivery systems are considered the safest and most effective by increasing the concentration of a therapeutic substance at the tumor site while decreasing it at other organs. Therefore, these delivery systems required lower doses for high therapeutic value with minimum side effects. The current review focuses on targeting therapeutic substances at the desired site using nanocarriers. Additionally, the diagnostic applications of nanocarriers in colorectal cancer are also discussed