Gefitinib (GFT) is a tyrosine kinase inhibitor drug used as a first-line treatment for patients with advanced or metastatic non-small cell lung, colon, and breast cancer. GFT exhibits low solubility and hence low oral bioavailability, which restricts its clinical application. One of the most important trends in overcoming such problems is the use of a vesicular system. Cubosomes are considered one of the most important vesicular systems used to improve solubility and oral bioavailability. In this study, GFT cubosomal nanoparticles (GFT-CNPs) were prepared by the emulsification method. The selected formulation variables were analyzed and optimized by full factorial design and response surface methodology. Drug entrapment efficiency (EE%), transmission electron microscopy, particle size, polydispersity index, in vitro release and its kinetics, and the effect of storage studies were estimated. The chosen GFT-CNPs were subjected to further investigations as gene expression levels of tissue inhibitors of metalloproteinases-1 (TIMP-1) and matrix metalloproteinases-7 (MMP-7), colon biomarkers, and histopathological examination of colon tissues. The prepared GFT-CNPs were semi-cubic in shape, with high EE%, smaller vesicle size, and higher zeta potential values. The in vivo data showed a significant decrease in the serum level of embryonic antigen (CEA), carbohydrate antigen 19-9 (CA 19-9), and gene expression level of TIMP-1 and MMP-7. Histopathological examination showed enhancement in cancer tissue and highly decreased focal infiltration in the lamina propria after treatment with GFT-CNPs.

In an effort to tackle the skin reactions frequently observed with topical application of ivermectin (IVM), a study was conducted to develop and optimize transethosomes (TESMs) loaded with IVM for scabies treatment. A three-factor, two-level (2³) full factorial design was employed. Soyabean phosphatidylcholine concentration (A), ethanol concentration (B) and Span 60 amount (C) were studied as independent factors, while entrapment efficiency (EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and drug release after 6 h (Q6h) were characterized. The skin sensitivity of the optimized formulation was evaluated by skin irritation test and histopathological examination. The EE% ranged from 88.55 ± 0.576% to 94.13 ± 0.305%, PS was from 318.033 ± 45.61 nm to 561.400 ± 45.17 nm, PDI was from 0.328 ± 0.139 to 0.671 ± 0.103, ZP was from −54.13 ± 1.09 mV to −60.50 ± 2.34 mV and Q6h was from 66.20 ± 0.30% to 93.46 ± 0.86%. The IVM-loaded transethosomal cream showed lower skin irritation and a more intact epidermal layer with intact keratinocyte, compared to the marketed cream which showed severe destruction of the keratin layer. Therefore, patient compliance can be improved by encapsulating IVM within TESMs to minimize its skin reactions.

Objective: The fundamental objective of this research investigation was to develop intravaginal diazepam (DZ)-loaded alginate beads for the management of acute pelvic floor dysfunction (PFD) pain with minimal sedative effect.Methods: DZ loaded beads were prepared by an ionotropic gelation method using SA (sodium alginate) alone, or in combination with either poloxamer 407 (PL), pectin (PC), or xanthan gum (XG) at different ratios in the presence of different concentrations of calcium chloride as a cross-linking agent. The successfully developed beads were evaluated for the particle size, pH, yield percentage, entrapment efficiency, in vitro bioadhesion, swelling percentage, and in vitro drug release. The stability, ex vivo drug permeation, and sedative action of the optimized beads formulations were studied.Results: The particle size of the formulated beads was from 395±3.3 to 515±2.8 μm, yield percentage was from 68.2±1.7 to 87.5±2.1, entrapment efficiency was from 65.6±1.6 to 87.5±2.1. pH ranged from 6.1±0.2 to 6.8±0.6, bioadhesion strength was from 71.5±1.3 to 87.6±3.1, and swelling percentage was in the range from 53.4±3.1 to 85.2±3.7. Approximately 92.4–72.6% of the loaded dose was released from the prepared beads. The optimized beads showed a good stability under the selected storage conditions. About 74.8%, 71.1%, 68.6%, and 63.4% of the loaded dose permeated through the rabbit vaginal mucosa from F7, F9, F3, and F11, respectively. The formulated beads decreased the sedative action associated with orally or parenterally administered DZ.Conclusion: The developed beads were considered a promising candidate to formulate DZ into a new dosage form for the treatment of PFD with a minimum central nervous system sedation.