Repurposing of nifedipine loaded in situ ophthalmic gel as a novel approach for glaucoma treatment.

Glaucoma is a chronic eye disease characterized by elevated intraocular pressure (IOP) which causes severe complications to the eyes and may lead to vision loss. The effective treatment of such diseases motivated the search for novel and unique drugs and delivery systems. It has been reported that, nifedipine (NF) is effective in reducing the elevated IOP due to vasodilatation of eye vascular smooth muscles. NF loaded thermo-sensitive in situ gels were prepared by the cold method using poloxamer 407 (P407) and hydroxypropyl methyl cellulose (HPMC) polymers adopting Box-Behnken experimental design. All the prepared formulae were tested for homogeneity, clarity, pH, isotonicity, gelling capacity, rheological behavior, in vitro drug release and were tested in vivo on rabbits. The prepared in situ gels were homogenous, transparent, having a pH ranged from 5 to 5.5 and undergo sol-gel transition within few seconds physiological temperature. The in situ gels showed sustained in vitro release of NF where about 76% of the loaded drug was released over 12 h. NF loaded in situ gels showed a 45.83 ± 2.91% reduction in the IOP, with no sign of toxicity or irritation to the eye in rabbits. The current investigations clarified the efficiency of this novel and unique NF loaded in situ gel for the control of the IOP compared to the conventional ophthalmic dosage forms.

Pimpinella anisum essential oil nanoemulsions against Tribolium castaneum-insecticidal activity and mode of action.

The red flour beetle, Tribolium castaneum Herbst (Coleoptera: Tenebrionidae), is an economically important pest of stored products. As possible alternative to conventional insecticides for its management, plant essential oils have gained interest owing to their effectiveness and eco-friendly features. However, they also show some drawbacks, such as low stability, poor water solubility and diffusion, and limited persistence in the environment. A good strategy to overcome these disadvantages is represented by green nanotechnologies. Herein, we developed a nanoemulsion based on the essential oil from Pimpinella anisum L. (Apiaceae) containing 81.2% of (E)-anethole and evaluated its toxicity on T. castaneum adults and F1 progeny, as well as its morphological and histological impact. The aniseed oil nanoemulsion was characterized by the formation of a semi-solid interphase between oil and water; mean drop size was 198.9 nm, PDI was 0.303, zeta potential was - 25.4 ± 4.47 mV, and conductivity was 0.029 mS/cm. The nanoemulsion showed toxicity on T. castaneum (LC50 = 9.3% v/v), with a significant impact on its progeny. Morphological and histological damages triggered by feeding and exposure to the aniseed nanoemulsion were analyzed by scanning electron microscopy (SEM) and light microscopy. Overall, our findings showed that the development of nanoemulsions allows to improve the stability of P. anisum essential oil enhancing its efficacy against stored grain pests and contributing to reduce the use of harmful synthetic insecticides.