The aim of the current manuscript was to test the applicability of a nanocomposite system of penetration enhancer vesicles (PEVs) within polymeric in situ forming gel network composed of poloxamer and hyaluronic acid for the intranasal delivery of the antiemetic dimenhydrinate (DMH). PEVs were prepared using phospholipids and labrasol/transcutol/PEG 400 as penetration enhancers, and characterized for entrapment efficiency (EE%), particle size, zeta potential and morphology. The nanocomposite in situ forming gel system was characterized for its sol-gel temperature, viscosity and mucoadhesiveness, and was pharmacodynamically tested on a cisplatin induced emesis model in rats in terms of food, water, kaolin intake and stomach weight content. The selected PEVs formula displayed EE% of 83% for DMH, particle size of 121 nm and a surface charge of 0.83 mV. The selected nanocomposite in situ gelling formula showed a viscosity of 2.13 Pa.S, mucoadhesive force of 0.62 N and DMH controlled release over 6 hours. The pharmacodynamic study showed the superiority of the nanocomposite in situ gelling formula; being administered at a lower dose than the oral marketed formula. The described nanocomposite system proved to be successful for the intranasal delivery of DMH, thus presenting a promising delivery modality for similar antiemetics.
Nutraceuticals have recently gained interest owing to their valuable contribution in the treatment of several diseases, with high safety margin and low incidence of side effects. However, their efficacy is limited by some challenges, namely poor solubility, low permeability, and, consequently, low bioavailability. Delivery carriers have proven that they can overcome almost all the aforementioned limitations, leading to improvement in the pharmacological efficacy of nutraceuticals. Among the promising nutraceuticals that have currently evoked considerable interest is mangiferin from mango tree, which is a polyphenol exhibiting many favorable pharmacological actions, but unfortunately suffers from poor aqueous solubility and other limitations that lower its bioavailability and halter its efficacy. This review summarizes the pharmacological actions of mangiferin and provides an insight on how delivery carriers for mangiferin (lipidic, vesicular, polymeric, inorganic, and protein nanoparticles, as well as complexes) can overcome its pharmaceutical challenges, hence reflecting on its improved therapeutic effects in treatment of different diseases.
Mangiferin (Mgf), a xanthone glucoside of natural origin, is well known to possess different pharmacological actions such as analgesic, antiviral, antidiabetic, anti-inflammatory, hepatoprotective, and antitumor. However, concerning water solubility it is sparingly soluble; in addition, it is classified as a BCS class IV compound which limits its bioavailability. Lipid nanocapsules (LNCs) are a promising carrier for oral delivery as it provides better solubility of the drug and enhances the drug absorption after oral administration owing to their small size. In this study, mangiferin-loaded lipid nanocapsules (Mgf-LNCs) were prepared using phase inversion temperature using solutol and cremophor RH40. This was followed by the characterization of the formed Mgf-LNCs by measuring particle size (PS), zeta potential (ZP), polydispersity index (PDI), in vitro release, viscosity, and stability after storage was also evaluated. The obtained results showed that PS for the prepared LNCs ranged from 22.88 ± 3.10 to 436.35 ± 69.37 nm. The ZP range of prepared LNCs was from -6.48 ± 2.13 to -1.90 ± 0.08 mV and showed a PDI ranging from 0.05 ± 0.01 to 0.72 ± 0.28 and viscosity ranging from 6.21 ± 2.90 to 1361.20 ± 92.21 mPa*s. The cumulative % release ranged from 48.89 ± 2.54 to 94.33 ± 9.63% after 6 hours period. After storage for 3 months in the refrigerator it is clear that the prepared formulae showed significant stability. Finally, it is concluded that LNCs are promising nanocarriers for the delivery of Mgf via the oral route.
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