In the present study, the biopotential of capsaicin (an active principle of capsicum) as a topical antiarthritic agent was studied in arthritic rats. Transfersomal vesicular system was employed for the topical administration of capsaicin in experimental rats. The characterization of prepared capsaicin-loaded transfersomes reveals their nano size (94 nm) with negative surface charge (-14.5 mV) and sufficient structural flexibility, which resulted in 60.34% entrapment efficacy, penetration across the biomembrane (220 µm) and 76.76% of drug release from vesicular system in 24 h in their intact form as evident from confocal laser scanning micrographic study. Results of transfersomal nanoformulation (capsaicin loaded, test) were compared with that of conventional gel formulation available in the market (Thermagel, standard), with an aim to assess the antiarthritic efficacy of our prepared capsaicin-loaded transfersomal formulation. In vivo antiarthritic activity study shows that our formulation possesses superior inhibitory activity than the marketed Thermagel formulation at the same dosage level, which could probably be due to the lesser permeability of Thermagel across the dermal barriers compared to our specially designed transfersomal delivery system. Moreover, the better tolerance of prepared vesicular formulation in biological system further enlightens the suitability of the transfersomal vesicle to be used as a novel carrier system for the topical administration of such highly irritant substance.
Long term tamoxifen citrate therapy is imperative to treat several dermatological and hormonal sensitive disorders. Successful oral and parenteral administration of tamoxifen citrate has been challenging since it undergoes enzymatic degradation and has poor aqueous solubility issues. In the present work, tamoxifen citrate loaded ethosomes were prepared and characterized for transdermal applications. The prepared formulations were characterized for morphological features, particle size distribution, calorimetric attributes, zeta potential and drug entrapment. Permeation profile of prepared ethosomes was compared with liposomes and hydroethonalic solution across cellophane membrane and human cadaver skin. Results of the permeation studies indicate that ethosomes were able to deliver >90% drug within 24 hours of application, while liposomes and hydroethanolic solution delivered only 39.04% and 36.55% respectively. Skin deposition and stability studies are also reported.
Cordia dichotoma Forst.has been used in the management of pain and inflammations in traditional medicine. However, the anti-inflammatory activity of the methanolic extract of C. dichotoma(MECD) bark has not been reported so far. This work was, therefore, aimed at investigating the anti-inflammatory activity of C. dichotomabark extract. The antioxidant activity was evaluated to justify the anti-inflammatory action of MECD on the basis of its radical scavenging property. The extract of C. dichotomawas obtained by Soxhlation of bark powder using methanol as solvent. The anti-inflammatory activity was determined by the carrageenan induced paw edemamodel in ratsat two different dose levels, viz., 250 and 500 mg/kg. The antioxidant activity was evaluated using DPPH radical scavenging assay. The antioxidant activity was performed in vitro by DPPH radical scavenging assay using ascorbic acid as the standard drug. In anti-inflammatory activity, maximum inhibition of edema was observed after 4 hours of experimental period. At lower test dose (250 mg/kg b.w.), the percentage inhibition of paw edema was 29.7 %, while 48.6 % inhibition of edema was observed at higher dose (500 mg/kgb.w.). The percentage inhibition of paw edema was significant relative to the control group. The standard indomethacin group also exhibited sufficiently high level of anti-inflammatory effect with 56% inhibition of paw edema at 5 mg/kg dose. In in vitroantioxidant activity, the MECD exhibited good DPPHradical scavenging activity with the IC50 vale of 62.46 µg/ml, whereas the standard drug, ascorbic acid showed comparatively more antioxidant activity with IC50 of 27.66 µg/ml.However, our study scientifically validates the folkloric claim as well as traditional uses of C. dichotomaas anti-inflammatory medication. It is suggested that the anti-inflammatory activity of C. dichotomamay be due to the antioxidant potential of phenolic phytoconstituents or plant flavonoids present in the methanolic bark extract.
The significant positive results, with reduced irritant effect of the semipurified capsaicinoids extract of Bhut Jolokia-loaded ethosomal nanovesicle carrier, suggest that it could be one of the choices for formulation development in anti-arthritic medicine.
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