Nanoemulsions (NE) are isotropic, dispersions of oil, water, surfactant(s) and cosurfactant(s). A range of components (11 surfactants, nine cosurfactants, and five oils) were investigated as potential excipients for preparation of ketorolac tromethamine (KT) ocular nanoemulsion. Diol cosurfactants were investigated for the effect of their carbon chain length and dielectric constant (DEC), Log P, and HLB on saturation solubility of KT. Hen’s Egg Test—ChorioAllantoic Membrane (HET-CAM) assay was used to evaluate conjunctival irritation of selected excipients. Of the investigated surfactants, Tween 60 achieved the highest KT solubility (9.89 ± 0.17 mg/mL), followed by Cremophor RH 40 (9.00 ± 0.21 mg/mL); amongst cosurfactants of interest ethylene glycol yielded the highest KT solubility (36.84 ± 0.40 mg/mL), followed by propylene glycol (26.23 ± 0.82 mg/mL). The solubility of KT in cosurfactants was affected by four molecular descriptors: carbon chain length, DEC, log P and HLB. KT solubility was directly proportional to DEC and the HLB yet, inversely proportional to carbon chain length and log P. All surfactants, except Labrasol ALF, were non-irritant. The majority of cosurfactants were slightly irritant, butylene glycol was a moderate irritant, pentylene and hexylene glycols were strong irritants. These findings will inform experiments aimed at developing NE formulations for ocular administration of KT.

خلفية البحث: لوليكونازول ، فئة جديدة من العامل المضاد للفطريات إيميدازول، وهو فعال للغاية ضد العديد من أنواع الفطريات، وبشكل كبيرالفطريات الجلدية. لديه قابلية منخفضة للذوبان في الماء تعمل كحاجز للتوصيل الموضعي وتحد من توافرها عن طريق الجلد. الاهداف: يهدف هذا البحث إلى صياغة مستحلب نانوي زيت/ماء لدواء اللوليكونازول بطريقة التسحيح المائي. المواد وطرق العمل: دراسة الذوبانية ينتج عنها اختيار زيت النعناع، توين 80 و ترانسكيوتول بي كطور زيتي، خافض للتوتر السطحي ومواد مساعدة لخفض التوتر السطحي على التوالي ،وفي نفس السياق أن المخططات مثلثة الشكل تبني منطقة مستحلب نانوي للصيغ المنتقاة. تم تحضير خمسة عشر صيغة زيت/ماء مستحلب نانوي وتم تقييمها من حيث حجم القطرة ، مؤشر التشتت المتعدد، قيم الأس الهيدروجيني، نسبة النفاذية و محتوى اللوليكونازول. من بين الصيغ، يتم إدخال ثمانية تركيبات لتحسين لزوجة مستحلب النانو المحضر عن طريق المزج مع 0.5% كاربوبول 934 كعامل يحدث التهلم. النتائج: هذه التركيبات المختارة اظهرت هلامات مستحلبة نانوية متجانسة مع قيم الأس الهيدروجيني المناسبة للاستعمال الجلدي ومحتوى لوليكونازول مقبول....

Buccal candidiasis has become increasingly prevalent in recent years, with Candida albicans being the primary causative organism. While systemic fluconazole is an effective treatment, its use is associated with adverse effects such as gastric upset, hepatic failure, and potential drug interactions. Therefore, the development of local fluconazole treatment presents a promising solution to these challenges. This study aimed to formulate an efficient local mucoadhesive film-forming spray for the targeted delivery of fluconazole in the treatment of oral candidiasis. The investigation involved the use of three polymers (hyaluronic acid, polyvinyl alcohol, and xanthan gum) both individually and in combination to identify the most effective formulation. Various tests were conducted to characterize 13 formulations prepared using these polymers, including UV-vis spectroscopy, Fourier-transform infrared spectroscopy (FTIR), content assay, drying time and film formation, viscosity determination, determination of the mucoadhesion strength by turbidimetric methods, drug release study, in-vitro anticandida activity, histological irritation analysis, and stability study. The optimum formula F11, comprised polyvinyl alcohol for its superior mechanical properties and film-forming capabilities, hyaluronic acid, and xanthan gum in combination, exhibiting synergistic mucoadhesive strength. This optimal formulation demonstrated maximum mucoadhesion, rapid film formation, an acceptable spray angle, and controlled release. Furthermore, the optimum formula underwent additional evaluations for in vitro anti-Candida activity, in vivo irritancy assessments, and stability studies, all of which yielded satisfactory results. These findings support the potential of the optimum formula as a straightforward and efficient spray formulation for the treatment of oral candidiasis.

Olanzapine (OLZ) is classified as a typical antipsychotic drug utilized for the treatment of schizophrenia. Its oral bioavailability is 60% due to its low solubility and pre-systemic metabolism. Hence, the present work aims to formulate and evaluate OLZ nanoparticles dissolving microneedles (MNs) for transdermal delivery to overcome the problems associated with drug administration orally. OLZ nanoparticles were prepared by the nanoprecipitation method. The optimized OLZ nanoparticle formula was utilized for the fabrication of dissolving MNs by loading OLZ nanodispersion into polydimethylsiloxane (PDMS) micromould cavities, followed by casting the polymeric solution of polyvinylpyrrolidone(PVP-K30) and polyvinyl alcohol (PVA) to form MN matrix. The results revealed that the optimized OLZ nanoparticle formula (NP-5) exhibited particle size 115.76±5.45 nm, entrapment efficiency 78.4±5.46, and zeta potential -19.01±1.6 mV. The results of MNs revealed that MN-4 exhibits a high drug content of 98.52%, and ex vivo permeation through rabbit skin exhibited that MN-4 permeates more effectively than a simple patch by approximately 5.16 fold. In vivo pharmacokinetics study revealed that the area under curve AUC 0-∞ of MN-4 was 6054.56±376 ng. h/ml as compared with AUC0-∞ of marketed OLZ tablet was 3975.77±373 ng. h/ml. It can be concluded that the dissolving MN-4 patch is considered a promising formula to overcome the problems associated with drug administration orally and could improve drug bioavailability, in addition to the ease of administering the medication to schizophrenic patients.

Introduction: Protein-based nanocarriers, particularly albumin nanoparticles (NPs), offer numerous advantages when compared to other nanomaterials. These carriers are characterized by biocompatibility, biodegradability, reduced immunogenicity, and decreased cytotoxicity. Moreover, proteins possess an inherent ability to target tumor cells directly or indirectly. Aim: This study aims to investigate the impact of various organic solvents on the characteristics of synthesized bovine serum albumin NPs (BSA NPs). Method: BSA NPs were produced using methanol, acetone, ethanol, dimethylsulfoxide (DMSO), and acetonitrile through the desolvation technique to achieve particles of acceptable size. Dynamic light scattering (DLS), blood compatibility assays, polyacrylamide gel electrophoresis (PAGE), and size exclusion chromatography (SEC) were employed to elucidate the properties of the generated NPs. The cytotoxicity of BSA NPs prepared under different conditions was assessed using Michigan Cancer Foundation - Mammary Adenocarcinoma - Breast Cancer 231 cells (MDA-MB-231 cells). Results: The particle size of the synthesized NPs varied based on the organic solvent utilized, with the smallest size of 114.2 nm observed with methanol. Blood compatibility results indicated no abnormal interactions between BSA NPs and blood components. PAGE analysis revealed a strong band near 72 kDa for untreated BSA and BSA treated with all organic solvents. In SEC, the retention time of native albumin was 6.65 min, while the average retention times of the prepared BSA NPs ranged from 5.14 to 5.21 min, showing similarity to the native protein. Except for NPs produced with methanol and acetonitrile, cytotoxicity testing on MDA-MB-231 cells demonstrated no significant harmful effects at various concentrations (0-500 μg/mL). Conclusion: The choice of desolvating agent significantly influences the size of BSA NPs. Various factors, such as solvent characteristics like hydrogen bonds, polarity, dielectric constant, and functional groups, can affect the particle size and structure of BSA NPs. The compatibility of cross-linked BSA NPs with blood components suggests their potential for intravenous drug delivery applications.

The novel Vierordt’s approach, or simultaneous equation method, was created and validated for the concurrent determination of vincristine sulfate (VCS) and bovine serum albumin (BSA) in pure solutions utilizing UV spectrophotometry. It is simple, precise, economical, rapid, reliable, and accurate. This method depends on measuring absorbance at two wavelengths, 296 nm and 278 nm, which correspond to the λ_max of VCS and BSA in deionized water, respectively. The calibration curves of VCS and BSA are linear at concentration ranges of 10–60 μg/mL and 200–1600 μg/mL, with correlation coefficient values (R²) of 1 and 0.999, respectively. The limits of detection (LOD) and quantification (LOQ) were 0.465 μg/mL and 1.410 μg/mL for VCS and 41.096 μg/mL and 124.533 μg/mL for BSA. The precision investigation indicated that the relative standard deviation (RSD) value was within limitations (RSD < 2%). The percentage recovery varied between 99.40 and 103.20% for VCS and 97.90 and 102.54% for BSA at various concentration levels, demonstrating that the simultaneous equation technique is accurate. The suggested approach can be successfully applied to estimate VCS and BSA simultaneously in pure and pharmaceutical-marketed products comprising these two components.