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In our study, the potential of bilosomes as novel vesicular carrier for the cutaneous delivery of the sulphone compound, Dapsone, for topical treatment of acne was investigated. The effect of different formulation variables (type and concentration of bile salt, and molar ratio of Span 60:cholesterol) on the properties of DPS-loaded bilosomes was investigated using a full factorial design. Design Expert software was used for data analysis and optimization of DPS-loaded bilosomes. The optimized bilosomes, chosen on the basis of their superior properties giving maximum entrapment, in vitro release after different time intervals and RE% with minimum vesicle size. Results showed that the bilosome system prepared using Span® 60: Cholesterol (5:1) and containing 0.25 M sodium deoxycholate as the bile salt was found to obey these criteria, with a desirability value of 0.637. Therefore, this system was chosen for further assessment for its morphological properties, zeta potential, thermal analysis using differential scanning calorimetry and X-ray diffractometry. Results revealed that the chosen bilosomes were spherical in shape with no aggregation, and contained DPS in a molecularly dispersed amorphous form. Finally, the capability of the optimized DPS-loaded bilosomes to deliver DPS through rat skin layers will be investigated and compared with that of DPS alcoholic solution. Results showed that the amounts of DPS retained in the skin treated with DPS-loaded bilosomes, and DPS alcoholic solution after 24 h were found to be 170.57 ± 55.12 and 120.24 ± 10.7 µg/mL, respectively, representing about 1.5-fold higher drug retained in the bilosomes-treated skin. Finally, the safety and the tolerability of the prepared bilosomes were assessed using histopathological examination, and revealed that the control untreated skin sections and skin sections treated with DPS-loaded bilosomes showed normal histological structures characterized by absence of defects or inflammation. Such results can be considered a good addition in the field of pharmaceutical drug delivery for effective topical therapy of acne. [ABSTRACT FROM AUTHOR]

Objectives: This study was aimed to develop dual-purpose natamycin (NAT)-loaded niosomes in ketorolac tromethamine (KT) gels topical ocular drug delivery system to improve the clinical efficacy of natamycin through enhancing its penetration through corneal tissue and reducing inflammation associated with Fungal keratitis (FK). Significance: Nanosized carrier systems, as niosomes would provide great potential for improving NAT ocular bioavailability.NAT niosomal dispersion formulae were prepared and then incorporated in 0.5%KT gels using different mucoadhesive viscosifying polymers. Methods: Niosomes were prepared using the reverse-phase evaporation technique. In vitro experimental, and in vivo clinical evaluations for these formulations were done for assessment of their safety and efficacy for treatment of Candida Keratitis in Rabbits. In vitro release study was carried out by the dialysis method. In vivo and histopathological studies were performed on albino rabbits. Results: NAT niosomes exhibited high entrapment efficiency percentage (E.E%) up to96.43% and particle size diameter ranging from 181.75 ± 0.64 to 498.95 ± 0.64 nm, with negatively charged zeta potential (ZP). NAT niosomal dispersion exhibited prolonged in vitro drug release (40.96–77.49% over 24h). NAT-loaded niosomes/0.5%KT gel formulae revealed retardation in vitro release, compared to marketed-product (NATACYN®) and NAT-loaded niosomes up to57.32% (F8). In vivo experimental studies showed the superiority for F8 in treatment of candida keratitis and better results on corneal infiltration and hypopyon level. These results were consistent with histopathological examination in comparison with F5 and combined marketed products (NATACYN® and Ketoroline®). Conclusions: This study showed that F8 has the best results from all pharmaceutical in vitro evaluations and a better cure percent in experimental application and enhancing the prolonged delivery of NAT and penetrating the cornea tissues. [ABSTRACT FROM AUTHOR]

Context:Muscle spasm is a painful involuntary contraction of muscles, which causes involuntary movement and distortion. Chlorzoxazone is a centrally acting muscle-relaxant with sedative properties, but given orally, it is hepatically metabolized leading to decreased bioavailability. Objective:Orodispersible tablets (ODTs) of chlorzoxazone were formulated using two different approaches; by coprocessed excipients (CE) or by liquisolid (LS) technique. Materials and methods:Pharmaburst®500, Starlac®, Pearlitol flash®, Prosolv®odt and F-melt®were used as coprocessed superdisintegrants, whereas in LS, Avicel®PH101, Microcelac®100 and Cellactose®80 were used as carriers, while Aerosil®200 was the coating material. ODTs were evaluated in terms of weight and thickness variations, drug content, hardness, friability, wetting time, dissolution, disintegration time (DT) and palatability. Results:In vitroDT of CE-ODTs ranged from 26.43 ± 1.693 s to >180 s, whereas it was between 25.42± 0.203 s to >180 s in LS-ODTs. Complete drug release within 15 min was attained by CE1 prepared with 92.5 mg Pharmaburst®500.In vivoDT of CE1 and LS3 were 19.779 ± 0.810 and 18.105 ± 0.423 s, respectively, using six volunteers. Volunteers found that CE1 had more acceptable taste and was more palatable than LS3. Conclusion:It was concluded that chlorzoxazone ODTs could be successfully formulated using either CE or LS techniques and be used as novel dosage forms for pediatrics and geriatrics showing improved drug release. Moreover, CE technique was superior to LS technique in terms of palatability. [ABSTRACT FROM AUTHOR]

Meloxicam (Mel) is a non-steroidal potent anti-inflammatory drug with effective analgesic effect for various situations; e.g. postoperative pain. The early systemic exposure to Mel and hence the rapid onset of pharmacological action is limited by its poor water solubility; a situation which may be more pronounced during acute pain episode because of reduced gastric motility that affects disintegration and dissolution of solid dosage forms. To overcome delayed absorption of Mel, improvement in the dissolution behavior of Mel is essential. Firstly, Mel spherical crystalline agglomerates (SCA) were prepared. Secondly, selected Mel SCA were integrated into intraoral fast disintegrating (OF) and edible (EF) films, they possess larger surface area that leads to rapid disintegration and release of the drug into the oral cavity within seconds and hence a rapid onset of action could be achieved. Stability study of formulations resulting in faster and higher extent of dissolution and suitable mechanical properties (G3 and G12) revealed their physical and chemical stability after three months of storage under different conditions. Both G3 and G12 successfully offered rapid absorption rate and accordingly an earlier systemic exposure to Mel compared to Mobic tablets as revealed by significantly earlierTmaxand higher AUC0–0.5hand AUC0–4h.Tmaxfollowing G3 fast disintegrating film administration was comparable to that reported following Mel parenteral administration but avoiding patient inconvenience. Both films may be suitable alternative to conventional oral and intramuscular Mel especially when earlier onset of action is required (in acute conditions). [ABSTRACT FROM AUTHOR]

Objective: Clonazepam (CP) is a potent long-acting nitrobenzodiazepine derivative that could be used for targeting peripheral benzodiazepine receptors. Phospholipid magnesome is a new vesicular nanosystem recently developed for brain targeting. Improving the uptake of 131 I-CP to the brain might be effective for the diagnosis and/or radiotherapy of certain brain diseases and/or tumors., Methods: CP was radiolabeled with 131 I using direct electrophilic substitution reaction. Quality control of 131 I-CP was performed using different techniques. Different formulas of 131 I-CP were prepared and characterized according to particle size and polydispersity index. The structural features of the optimized formula were then interpreted using transmission electron microscopy and scanning electron microscopy, whereas pharmacokinetic and in vivo behaviors were estimated using the intravenous and intranasal delivery routes., Results: The heart and blood demonstrated lower uptake of 131 I-CP, which inevitably decreased the nontarget effects of radioiodine. Intranasally administered 131 I-CP-loaded magnesomes (INMg) had noticeably higher brain uptake (7.1 ± 0.09%ID/g) with rapid onset of action within 5 min and effective pharmacokinetic behavior. INMg had a drug targeting efficiency and nose-to-brain direct transport percentage of 121.1% and 94.6%, respectively as well as a relative bioavailability of 441.04 ± 75.5%., Conclusion: The present study showed that 131 I-CP-loaded magnesomes can be a beneficial brain-targeting approach for improving the diagnosis and/or radiotherapy of certain brain diseases., (Copyright © 2021. Published by Elsevier B.V.)