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Diabetes mellitus is a life-threatening metabolic disease. At the moment, there is no effective treatment available to combat it. In this study, we aimed to develop berberine-loaded bilosomes (BER-BLS) to boost the oral bioavailability and therapeutic efficacy of berberine, a natural antidiabetic medication. The BER-BLS was fabricated using a thin-film hydration strategy and optimized using a central composite design (face-centered). The average vesicle size, entrapment efficiency, and surface charge of the optimized BER-BLS preparation were 196.5 nm, 89.7%, (-) 36.4 mV, respectively. In addition, it exhibited higher stability and better-sustained release of berberine than the berberine solution (BER-SOL). BER-BLS and BER-SOL were administered to streptozocin-induced diabetic rats. The optimized BER-BLS formulation had a significant hypoglycemic impact, with a maximum blood glucose decrease of 41%, whereas BER-SOL only reduced blood glucose by 19%. Furthermore, the pharmacological effect of oral BER-BLS and BER-SOL corresponded to 99.3% and 31.7%, respectively, when compared to subcutaneous insulin (1 IU). A pharmacokinetic analysis found a 6.4-fold rise in the relative bioavailability of berberine in BER-BLS when compared to BER-SOL at a dosage of 100 mg/kg body weight. Histopathological investigation revealed that BER-BLS is suitable for oral administration. Our data demonstrate that BLS is a potential nanocarrier for berberine administration, enhancing its oral bioavailability and antidiabetic activity. [ABSTRACT FROM AUTHOR]

Asthma represents a globally serious non-communicable ailment with significant public health outcomes for both pediatrics and adults triggering vast morbidity and fatality in critical cases. The ß2-adrenoceptor agonist, terbutaline sulfate (TBN), is harnessed as a bronchodilator for monitoring asthma noising symptoms. Nevertheless, the hepatic first-pass metabolism correlated with TBN oral administration mitigates its clinical performance. Likewise, the regimens of inhaled TBN dosage forms restrict its exploitation. Consequently, this work is concerned with the assimilation of TBN into a novel non-phospholipid nanovesicular paradigm termed novasomes (NVS) for direct and effective TBN pulmonary targeting. TBN-NVS were tailored based on the thin film hydration method and Box-Behnken design was applied to statistically optimize the formulation variables. Also, the aerodynamic pattern of the optimal TBN-NVS was explored via cascade impaction. Moreover, comparative pharmacokinetic studies were conducted using a rat model. TBN elicited encapsulation efficiency as high as 70%. The optimized TBN-NVS formulation disclosed an average nano-size of 223.89 nm, potential of -31.17 mV and a sustained drug release up to 24 h. Additionally, it manifested snowballed in vitro lung deposition behavior in cascade impactor with a fine particle fraction of 86.44%. In vivo histopathological studies verified safety of intratracheally-administered TBN-NVS. The pharmacokinetic studies divulged 3.88-fold accentuation in TBN bioavailability from the optimum TBN-NVS versus the oral TBN solution. Concisely, the results proposed that NVS are an auspicious nanovector for TBN pulmonary delivery with integral curbing of the disease owing to target specificity. [ABSTRACT FROM AUTHOR]

Three sensitive and cost-effective spectrophotometric methods are introduced for the determination of amoxicillin and dicloxacillin in their binary mixtures with minimum sample pretreatment, with or without the presence of their common impurity; 6-aminopenicillanic acid (6-APA). In this work, dicloxacillin is determined by dual wavelength, derivative ratio and isoabsorptive spectrophotometric methods. However, amoxicillin is determined by direct UV spectrophotometry at 273.6 nm and by the first derivative ratio spectrophotometric method (DD method). For method (A); the dual wavelength method, the wavelengths selected for the determination of dicloxacillin were 223.6 and 237 nm. Method (B); the isoabsorptive spectrophotometric method, comprises measuring the total content of the mixture at their isoabsorptive point (230.4 nm), and then the content of dicloxacillin can be calculated by subtraction. Method (C) is the first derivative of ratio spectra for the determination of amoxicillin (using 8 μg/mL of dicloxacillin as a divisor at 231 nm) and dicloxacillin (using 20 μg/mL of 6-APA as a divisor at 234.6 nm) in presence of their common impurity; 6-APA. Statistical comparison of the results obtained from the suggested methods with those of the reported HPLC method showed no significant difference with respect to accuracy and precision. The developed methods can be used for quality control analysis of the studied drugs in laboratories lacking HPLC qualifications. Kay words: Amoxicillin, Dicloxacillin, Dual wavelength, Isoabsorptive point, First derivative ratio [ABSTRACT FROM AUTHOR]