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Brimonidine
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Brimonidine is a quinoxaline derivative and a selective α2-adrenergic receptor agonist. Upon ocular administration, brimonidine acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor; it also enhances its outflow. Brimonidine ophthalmic solution is indicated for patients with open- angle glaucoma or ocular hypertension to lower intraocular pressure. A topical gel is indicated for the treatment of persistent facial erythema of rosacea in adults, where it reduces erythema through direct vasoconstriction. In pharmaceutical products, brimonidine is employed as brimonidine tartrate (CAS number 70359-46-5, EC number not available, molecular formula C15H16BrN5O6) (1).
Nanocarriers Systems and Their Application for the Delivery of Different Phytoconstituents
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Ebru Altuntaş, Gülgün Yener, Burcu Özkan
Luteolin (LUT) is an encouraging molecule also with anti-arthritic effects. Abidin et al. (2016) designed niosomal topical gel for improved transdermal penetration of LUT. Different non-ionic surfactants (Span-60, Span-40, Tween-80, Tween-20) and vesicle type delivery systems were used for formulation of niosomes. According to the vesicle size measurement, all vesicles were found to be in the range between 534.58–810.22 nm, which is accepted as favorable for transdermal penetration of drugs. The LUT yield in vesicles was evaluated to be higher with all surface actives (maximum; 89.12 ± 3.12 and minimum; 67.83 ± 0.29). The chosen formulation exhibited spectacular results regarding to drug penetration capacity with an improvement degree of 2.66 when checked against control formulation. The in vivo bioavailability studies showed that novel niotransgel of LUT had the ability to ensure anti-arthritic efficacy, and the findings were comparable to the marketed diclofenac gel. In conclusion, the findings have been proven by radiological analysis, which confirmed that the newly prepared niosomal transdermal gel formulation was sufficiently able to treat arthritis and findings could be accepted satisfactory when compared with the standard.
Designed Antimicrobial Peptides: A New Horizon
Published in Heather A.E. Benson, Michael S. Roberts, Vânia Rodrigues Leite-Silva, Kenneth A. Walters, Cosmetic Formulation, 2019
Kathryn W. Woodburn, Chia-Ming Chiang, Jesse Jaynes, L. Edward Clemens
The importance of the right formulation and delivery method in topical pharmaceuticals is critical. The optimal formulation for topical delivery of dAMP is determined by the properties of the dAMP, the selected excipients, type of formulations and the target sites. Given the hydrophilic properties of the dAMPs and the direct cytolytic action of the dAMPs with minimal eukaryotic toxicity, topical gel formulations are commonly used for dAMP administration when targeted for skin indications.
Development of topical thymoquinone loaded polymer–lipid hybrid vesicular gel: in-vitro and ex-vivo evaluation
Published in Journal of Liposome Research, 2022
Sagar Trivedi, Kamlesh Wadher, Milind Umekar
The viscosity of the gel is the rheological behaviour of topical/transdermal formulations and has a profound effect on the spreadability of the formulation, its retention, and contact time on the skin surface (Junyaprasert et al.2008, Hashemzadeh et al.2020). Hence the effect of concentration of Carbopol gel containing TH PLH vesicular gel formulation viscosity profile was studied. The 1% w/v TH PLH vesicular-Carbopol gel demonstrated high viscosity having maximum shear stress of 6110 cP and minimum shear stress of 18680 cP. The above result shows the shear-thinning properties (pseudoplastic nature) of the prepared formulation, which facilitates ideal properties of dermal formulations as they must exhibit thin during application and thick otherwise. The ideal viscosity of the vesicular gel was due to the sudden increase in the cross-linking of the polymer network of Carbopol at 1% w/v. The ideal topical gel must have a proper flow and smooth spreading ability at the position of application and that can be achieved by excellent spreading property.
Formulation and evaluation of butenafine loaded PLGA-nanoparticulate laden chitosan nano gel
Published in Drug Delivery, 2021
Sultan Alshehri, Syed Sarim Imam
The pH of BT-NPopG was found to be 6.6 ± 0.3, which is ideal for the topical formulation and does not produce any irritation (Riaz et al., 2020). The viscosity was also assessed to check the flow property of the prepared gel and the value was found to be 35,276 ± 14 cps. The viscosity lies between 35,000 and 40,000 cps is ideal for topical preparation, which gives good flow property and spreadability (Ahmed et al., 2021). The optimum viscosity value gives better adherence to the skin and spreadability. The viscosity of the gel also depends on the particle size and PDI value. The larger particle size gives higher viscous gel (Koca et al., 2018). The spreadability and extrudability of BT-NPopG were measured and the result showed 10.76 ± 1.09 cm and 14.98 ± 1.78 g/cm2, respectively. A good spreadability and extrudability value were found due to the optimum viscosity of the gel. The optimum viscosity and spreadability of topical gel can easily be applied to the skin in the form of a thin layer (Motawea et al., 2018).
Fabrication of moxifloxacin HCl-loaded biodegradable chitosan nanoparticles for potential antibacterial and accelerated cutaneous wound healing efficacy
Published in Journal of Microencapsulation, 2022
Misbah Hameed, Akhtar Rasul, Sumera Latif, Maria Rasool, Ghulam Abbas, Muhammad Irfan Siddique, Muhammad Khurram Waqas, Ikram Ullah Khan, Abid Mehmood Yousaf, Pervaiz Akhtar Shah
NPs of MXF HCl coated with chitosan were successfully prepared and loaded in a gel formulation for topical use in wound healing and as an antibacterial agent. High drug entrapment (63.5%) was obtained using 2:1 of chitosan and TPP. Prepared MXF NPs have a mean particle size of 359 ± 79 with +31.01 zeta potential and low PDI (00.8). In vitro release and antibacterial studies confirmed that NP-loaded formulation has better release at acidic pH 5.5 (83 ± 3.5%). In comparison, at pH 7.4, it is 74% with enhanced antimicrobial activity against two test organisms i.e. E. coli and S. aureus. In vivo wound healing studies suggests it can be used effectively as a topical gel for potential wound healing.