Injectable PLGA Adefovir microspheres; the way for long term therapy of chronic hepatitis-B.

For patient convenience, sustained release Adefovir Poly-d,l-lactic-co-glycolic acid (PLGA) microspheres were formulated to relieve the daily use of the drug which is a problem for patients treated from chronic hepatitis-B. PLGA microspheres were prepared and characterized by entrapment efficiency, particle size distribution and scanning electron microscopy (SEM). In-vitro release and in-vivo studies were carried out. Factors such as drug: polymer ratio, polymer viscosity and polymer lactide content were found to be important variables for the preparation of PLGA Adefovir microspheres. Fourier transform infrared (FTIR) analysis and differential scanning calorimetry (DSC) were performed to determine any drug-polymer interactions. One way analysis of variance (ANOVA) was employed to analyze the pharmacokinetic parameters after intramuscular injection of the pure drug and the selected PLGA microspheres into rats. FTIR and DSC revealed a significant interaction between the drug and the polymer. Reports of SEM before and after 1 and 24 h release showed that the microspheres had nonporous smooth surface even after 24 h release. The entrapment efficiency ranged between 55.83 and 86.95% and in-vitro release studies were continued for 16, 31 and 90 days. The pharmacokinetic parameters and statistical analysis showed a significant increase in the Tmax, AUC0-t and MRT, and a significant decrease in the Cmax of the tested formulation (p < 0.05). Results demonstrated that PLGA Adefovir microspheres could be used for long-term treatment of chronic hepatitis-B instead of the daily dose used by the patient.

Serum Sclerostin Level Among Egyptian Rheumatoid Arthritis Patients: Relation to Disease Activity, Bone Mineral Density and Radiological Grading.

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INTRODUCTION: Bone loss in rheumatoid arthritis is caused by increased bone resorption without increasing bone formation. The Wnt pathway is important in the control of bone formation through the regulation of osteoblast activity. Sclerostin is an important regulator of the Wnt pathway by blocking Wnt binding to its receptor and thereby inhibiting bone formation. AIM: This study aimed to assess the serum sclerostin level in a group of Egyptian rheumatoid arthritis patients and to correlate its level with bone mineral density, disease activity and radiological grading. METHODS: Forty rheumatoid arthritis patients (mean age 48.9 ± 11.6 years, disease duration 8 ± 6.4 years) and 40 age and sex matched apparently healthy subjects were included. Serum sclerostin level was measured using Enzyme linked Immunosorbent Assay. Plain radiographs of hands and feet and dual-energy x-ray absorptiometry test were done for all patients. RESULTS: No significant difference was found between rheumatoid arthritis patients and healthy controls as regard mean value of sclerostin level. Postmenopausal healthy women had higher levels of sclerostin than premenopausal healthy women only. Serum sclerostin had significantly positive correlations with the age of onset and weight of rheumatoid arthritis patients and negative correlation with Erythrocyte Sedimentation Rate. No correlation was encountered between sclerostin level and bone mineral density, disease activity or radiographic grading. CONCLUSION: For better clarification of the role of sclerostin on bone mass in rheumatoid arthritis, larger sample size is needed. More studies on serum sclerostin levels among different grades of RA activity are encouraged.