May Almukainzi1, Thanaa A El-Masry2, Walaa A Negm3, Engy Elekhnawy4, Asmaa Saleh1,5, Ahmed E Sayed6, Mohamed A Khattab7, Dalia H Abdelkader8. 1. Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah Bint Abdulrahman University, Riyadh, Saudi Arabia. 2. Pharmacology and Toxicology Department, Faculty of Pharmacy, Tanta University, Tanta, Egypt. 3. Pharmacognosy Department, Faculty of Pharmacy, Tanta University, Tanta, Egypt. 4. Pharmaceutical Microbiology Department, Faculty of Pharmacy, Tanta University, Tanta, Egypt. 5. Department of Biochemistry, Faculty of Pharmacy, Al Azhar University, Cairo, Egypt. 6. Faculty of Medicine, Tanta University, Tanta, Egypt. 7. Department of Cytology and Histology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt. 8. Pharmaceutical Technology Department, Faculty of Pharmacy, Tanta University, Tanta, Egypt.
Abstract
Purpose: Gentiopicroside (GPS), an adequate bioactive candidate, has a promising approach for enhancing wound healing due to its antioxidant and antimicrobial properties. Its poor aqueous solubility negatively affects oral absorption accompanied by low bioavailability due to intestinal/hepatic first-pass metabolism. Our aim in this study is to fabricate GPS into appropriate nanocarriers (PLGA nanospheres, NSs) to enhance its solubility and hence its oral absorption would be improved. Methods: Normal and ODS silica gel together with Sephadex LH20 column used for isolation of GPS from Gentiana lutea roots. Crude GPS would be further processed for nanospheres fabrication using a single o/w emulsion solvent evaporation technique followed by in vitro optimization study to examine the effect of two formulation variables: polymer (PLGA) and stabilizer (PVA) concentrations on the physical characterizations of prepared NSs. Possible GPS-PLGA chemical and physical interactions have been analyzed using Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The optimum GPS-PLGA NSs have been chosen for antimicrobial study to investigate its inhibitory action on Staphylococcus aureus compared with unloaded GPS NSs. Also, a well-designed in vivo study on streptozotocin-induced diabetic rats has been performed to examine the wound healing effect of GPS-PLGA NSs followed by histological examination of wound incisions at different day intervals throughout the study. Results: The optimum GPS PLGA NSs (F5) with well-controlled particle size (250.10±07.86 nm), relative high entrapment efficiency (83.35±5.71), and the highest % cumulative release (85.79±8.74) have increased the antimicrobial activity as it exhibited a higher inhibitory effect on bacterial growth than free GPS. F5 showed a greater enhancing impact on wound healing and a significant stimulating effect on the synthesis of collagen fibers compared with free GPS. Conclusion: These findings demonstrate that loading GPS into PLGA NSs is considered a promising strategy ensuring optimum GPS delivery for potential management of wounds.
Purpose: Gentiopicroside (GPS), an adequate bioactive candidate, has a promising approach for enhancing wound healing due to its antioxidant and antimicrobial properties. Its poor aqueous solubility negatively affects oral absorption accompanied by low bioavailability due to intestinal/hepatic first-pass metabolism. Our aim in this study is to fabricate GPS into appropriate nanocarriers (PLGA nanospheres, NSs) to enhance its solubility and hence its oral absorption would be improved. Methods: Normal and ODS silica gel together with Sephadex LH20 column used for isolation of GPS from Gentiana lutea roots. Crude GPS would be further processed for nanospheres fabrication using a single o/w emulsion solvent evaporation technique followed by in vitro optimization study to examine the effect of two formulation variables: polymer (PLGA) and stabilizer (PVA) concentrations on the physical characterizations of prepared NSs. Possible GPS-PLGA chemical and physical interactions have been analyzed using Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The optimum GPS-PLGA NSs have been chosen for antimicrobial study to investigate its inhibitory action on Staphylococcus aureus compared with unloaded GPS NSs. Also, a well-designed in vivo study on streptozotocin-induced diabetic rats has been performed to examine the wound healing effect of GPS-PLGA NSs followed by histological examination of wound incisions at different day intervals throughout the study. Results: The optimum GPS PLGA NSs (F5) with well-controlled particle size (250.10±07.86 nm), relative high entrapment efficiency (83.35±5.71), and the highest % cumulative release (85.79±8.74) have increased the antimicrobial activity as it exhibited a higher inhibitory effect on bacterial growth than free GPS. F5 showed a greater enhancing impact on wound healing and a significant stimulating effect on the synthesis of collagen fibers compared with free GPS. Conclusion: These findings demonstrate that loading GPS into PLGA NSs is considered a promising strategy ensuring optimum GPS delivery for potential management of wounds.
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