DEVELOPMENT AND EVALUATION OF CLOBETASOL–LOADED SOLID LIPID NANOPARTICLES FOR TOPICAL TREATMENT OF PSORIASIS

Objective: The current research was structured to achieve a maximum topical delivery for the drug clobetasol-17-propionate (CP) and to predict the effects of various independent variables like lipid: drug ratio, surfactant, and homogenization time on particulate characters and performance solid lipid nanoparticles (SLNs). Methods: CP loaded SLNs were formulated by Emulsification–Homogenization method and optimized using 33 full factorial designs (Design-Expert software 11.0). Drug loaded SLNs were evaluated for various parameters like particle size, surface charge, polydispersity index, entrapment efficiency, surface morphology, thermal analysis, in vitro drug release through skin (Franz diffusion cell), drug deposition study and stability. Results: The optimized formulation (SLNs) attains a minimal Particle size of 133.3±3.66 nm, Poly dispersibility index of 0.179±0.081, % entrapment efficiency of 78.1±1.11 and Zeta potential of-36.2±0.11mV. Skin permeation study of CP loaded SLNs suspension showed prolonged drug release up to 24h. Maximum drug deposition was obtained after developing the drug into SLNs (48.22µg/ml) when compared to the pure drug (19.12µg/ml). Conclusion: SLNs were promising colloidal particulate carriers by which prolonged drug release and improved skin permeation was achieved for the drug Clobetasol 17- propionate

EVALUATION OF ANTIPSORIATIC ACTIVITY OF AQUEOUS EXTRACT OF BRASSICA OLERACEA VAR. CAPITATA AND ETHANOLIC EXTRACT OF MENTHA SPICATA LEAVES ON IMIQUIMOD-INDUCED PSORIASIS-LIKE DERMATITIS

Objective: The objective of this study is to evaluate the antipsoriatic activity of aqueous extract of Brassica oleracea var. capitata leaves (BOAE) and ethanolic extract of Mentha spicata leaves (MSEE) on Imiquimod-induced Psoriasis-like dermatitis. Methods: Imiquimod induction method for psoriasis-like dermatitis was used for the evaluation of antipsoriatic activity. Extracts were tested at a dose of 100 mg/kg body weight (b.wt.) and 400 mg/kg b.wt. in Swiss albino mice. These test doses were compared with the Retino-A (0.025%) treated group which serves as a standard group. Parameters studied in the test include changes in body weight, spleen weight and spleen index, neutrophils, lymphocytes, eosinophils, monocytes, hemoglobin, red blood cells, platelets, packed cell volume, mean corpuscular volume, mean corpuscular hemoglobin (MCH), MCH concentration, epidermal thickness, erythema, desquamation, skin thickness, superoxide dismutase, catalase, lipid peroxidation of skin and percentage orthokeratotic values, drug activity, and relative epidermal thickness. Results: MSEE at dose of 400 mg/kg b.wt has shown more effect when compared with MSEE at low dose, BOAE topical and oral. Conclusion: From the study, it was concluded that the above extracts have promising anti-psoriatic activity

Antidepressant activity of ethanolic extract of oleo gum resins of Ferula asafoetida Linn

Objective. The study was undertaken to evaluate the antidepressant activity of ethanolic extract of Ferula asafoetida oleo gum resins. Materials and Methods. Five groups of rats (180–200g) and mice (20–30g) of both genders, each group comprising six animals, were used (i.e., normal, positive control, standard, FAEE 200mg/kg, and FAEE 400mg/kg treated groups). Forced swimming test (FST), Tail suspension test (TST), Potentiation of Norepinephrine-Induced Toxicity (PNEIT), Haloperidol- Induced Catalepsy (HIC), and Reserpine-Induced Hypothermia (RIH), were used as the validate models of depression in rodents. The study was confirmed by brain monoamines estimation (i.e. Dopamine, Norepinephrine and 5-HT), MAO levels and invivo antioxidant studies (CAT and SOD). Results. FAEE treated animals showed a significant and dose dependent effect on a decrease in immobility time in FST, TST, and decrease in catalepsy time in HIC. FAEE and imipramine (15mg/kg) showed a significant increase in body temperature in RIH, and also showed a potent lethality in PNEIT. FAEE treated animals showed a significant increase in the levels of brain monoamines, in vivo antioxidants, and a significant decrease in MAO levels. Conclusion. Results of present study indicate that FAEE has potent antidepressant-like activity, and this effect may be due to the anti-oxidant property of Ferulic acid and umbelliferone, or may be due to neuroprotective activity of other major phytoconstituents, e.g. flavonoids, phenolic acids and polysulfide compounds. To identify the particular compound responsible for the antidepressant-like activity required further molecular level studies

Evaluation of anti-fibrotic activity of ethanolic extract of Nelumbo nucifera gaertn. Seed against doxorubicin and unilateral ureter obstruction-induced renal fibrosis

Objective. The study were undertaken to evaluate anti-fibrotic activity of ethanolic extract of Nelumbo nucifera seed (NNSEE) against doxorubicin and Unilateral Ureter Obstruction-induced renal fibrosis. Materials and method. Animals were divided into five groups with six animals in each group, i.e. Normal, Positive control, Standard (Pirfenidone 200mg/kg), Test-I (NNSEE 200mg/kg), and Test-II (NNSEE 400mg/kg). Renal fibrosis was developed by doxorubicin and UUO-induced methods. After induction of renal fibrosis, profibrotic responses in biochemical parameters were observed, e.g. BUN, serum creatinine levels were elevated, while total protein and GFR levels decreased. Antioxidant (SOD and CAT) levels are also attenuates and hyalinized glomeruli cells, damage to tubular cells were noted in histopathology, which are all responsible for the development of renal fibrosis. Results. The result showed that the anti-fibrotic activity of NNSEE at a dose of 200 and 400mg/kg b.wt was comparable with the standard treatment 200mg/kg b.wt of pirfenidone (anti-fibrotic drug). These data supplemented with histopathological studies of rat kidney sections. NNSEE had reversed all the manifestation of renal fibrosis. Conclusion. Results of the study indicate that the NNSEE has potent anti-fibrotic activity, as well as antioxidant property, in dose dependent manner that may be due to the presence of major phytochemical constituents such as alkaloids, polyphenols

Powder X-ray Diffraction as an Emerging Method to Structurally Characterize Organic Solids

The current level of laboratory instrumentation and computational resources allows X-ray powder diffraction to be implemented into the toolbox of organic chemists, providing a means for rapid (i.e., within a day) structural characterization of organic solids, without the need for single crystals. We illustrate such use of powder diffraction using two case studies of molecular cocrystals of trifluoroacetic acid and malonic acid, involving theobromine, a model active pharmaceutical ingredient. We also report on a previously unobserved conformation of malonic acid in the solid state