Background: Melasma is one of the common pigmentary problems affecting females in our community, owing to the frequent use of hormonal contraceptives as well as our sunny climate. A lot of treatment options are available but none of them is completely satisfactory. Many patients prefer the use of topical preparations and minimally invasive methods. Tranexamic acid (TA) is a potential treatment option for hyperpigmentation with different delivery routes. Aim:We designed the study in order to evaluate the efficacy of TA in melasma using 2 different routes of delivery.Patients and methods: A randomised clinical trial was performed on 60 female patients with melasma, they randomly divided into three groups; A, B and C. Group (A) patients received TA (4 mg/mL) intradermal injections every 2 weeks with, group B received TA (10 mg/mL) intradermal injections every 2 weeks, group C received TA cream (10% concentration) twice daily, treatment continued for 12 weeks in all groups. Melasma Area and Severity Index (MASI) scores were measured for each patient before and after completion of treatment. Results:The percentage of MASI score reduction was highest in group B (62.7%) versus (39.1%) in group A, while the percentage of MASI reduction was the lowest in group C (4.2%). Conclusion:Tranexamic acid is a safe effective and well-tolerated treatment option for melasma patients. Intradermal injection of TA leads to better results than the topical application. Topical TA cream (even in a high concentration) produce fair improvement of melasma.

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5-Fluorouracil is widely used for treatment of colorectal cancer and is provided as intravenous bolus or infusion because it has erratic oral bioavailability. Diarrhea and myelosuppression are potential and the major side effects of the intravenous administration route. This work was aimed to develop colon-targeted delivery of 5-Fluorouracil microsponges so that, the oral bioavailability enhanced and the side effects could be potentially reduced. Quassi-emulsion solvent diffusion method was used to prepare 5-Fluorouracil microsponges using polyethylene glycol as an emulsifier. Different formulae were prepared with different composition and processing factors. The entrapment efficiency 5-Fluorouracil in these formulae ranged from 17.81 to 78.61%, the particle size of the prepared microsponges ranged from 87 to 229 µm and the % cumulative drug released after 24 hours ranged from 47.7 to 98.58%. The prepared microsponges were subjected to compatibility studies as Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Thus 5-fluorouracil microsponges considered as a promising system for the colon-specific delivery that has potential for future use as an anticancer therapy for colorectal cancer.

Simvastatin (SV) is a poorly soluble drug; its oral administration is associated with a significant problem: Myopathy. The present study aims to formulate SV microsponges that have the potential to minimize the myotoxicity accompanying the oral administration of the drug. SV microsponges were prepared by exploiting the emulsion solvent evaporation technique. The % entrapment efficiency (%EE) of the drug approached 82.54 ± 1.27%, the mean particle size of SV microsponges ranged from 53.80 ± 6.35 to 86.03 ± 4.79 µm in diameter, and the % cumulative drug release (%CDR) of SV from microsponges was significantly higher than that from free drug dispersion much more, the specific surface area of the optimized microsponges formulation was found to be 16.6 m2/g revealed the porosity of prepared microsponges. Histological and glycogen histochemical studies in the skeletal muscles of male albino rats revealed that microsponges were safer than free SV in minimizing myotoxicity. These findings were proven by Gene expression of Mitochondrial fusion and fission (Mfn1) & (Fis1) and (Peroxisome proliferator-activated receptor gamma co-activator 1α) PGC-1α. Finally, our study ascertained that SV microsponges significantly decreased the myotoxicity of SV.

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