Evaluation of Conocarpus erectus against multidrug resistant Staphylococcus aureus: Cell to animal study.

Antibiotic resistant infections by Staphylococcus aureus (S. aureus) in high risk patients is critical challenge for all clinicians across globe. In an effort to achieve robust bactericidal effect, therapeutic approach based on antimicrobial plant extract of Conocarpus erectus (C. erectus) been assessed in-vitro and in-vivo against S. aureus resistant clinical strains isolated from burn patients and antibiotic susceptibility was conducted using Kirby-baur disc diffusion technique. C. erectus plant extract obtained and characterized for phytochemical constituents, its hemocompatibility and for antioxidant potential. Minimum inhibitory concentration studied for C. erectus extract against multidrug resistance (MDR) S. aureus clinical isolates in-vitro and in rat's sepsis model. Therapeutic activity along acute toxicity was evaluated in rat's model. C. erectus extract showed marked antioxidant activity attributed to its phenolic components predominately along others. Hemocompatibility results were significantly different (p<0.05) compared to vancomycin (positive control). Statistically significant reduction in bacterial colony count (p<0.05) observed in rat's sepsis model with C. erectus treated group vs. controls. C. erectus extract offered higher bactericidal effect both in-vitro and in-vivo along no acute toxicity at therapeutic dose. We infer that it can serve as alternative promising treatment option against antibiotic resistant against MDR S. aureus strains.

Fixed Dose Single Tablet Formulation with Differential Release of Amlodipine Besylate and Simvastatin and Its Pharmacokinetic Profile: QbD and Risk Assessment Approach.

PURPOSE: A differential release fixed dose matrix tablet of amlodipine besylate (AML-B) and simvastatin (SIM) was formulated to enhance patient compliance. MATERIAL AND METHOD: In the first phase, release controlling parameters of AML-B and SIM granules were identified and in the second phase a fixed dose AML-B and SIM tablet formulation was prepared and optimized for a differential release of the drugs using a quality by design (QbD) and risk assessment approach. A validated HPLC method was employed for simultaneous determination of AML-B and SIM for FDC formulation. A pharmacokinetics of the above drugs was studied in healthy dogs in the third phase. RESULTS: In QbD-based optimized formulation, Eudragit® RSPO-dicalcium phosphate (DCP) blend controlled the release of AML-B over 8 h, though this diffusion-controlled release assumed first order kinetics. DCP and Eudragit® RS 100 also retarded release of SIM causing SIM release over 8 h after AML-B release from the optimized FDC tablet formulation. The HPLC retention times of AML-B and SIM were 2.10 and 15.52 min, respectively. Linearity for AML-B was 5.0-50 ng/mL and 0.01-2.0 µg/mL for SIM with percent recoveries of 92.85-101.53% and 94.51-117.75% for AML-B and SIM. AUC0-∞ of AML-B was increased 3 fold, while AUC0-∞ of SIM was decreased 2 fold. The tmax values for AML-B and SIM were 12 and 6 h, respectively. AML-B was absorbed without any lag time (tlag) while tlag was 6.33 ± 0.81 h for SIM, thus met the study objective. CONCLUSION: The pharmacokinetic study showed an immediate absorption of AML-B while that of SIM was withheld for 6 h, close to the desired delay time of 8 h.

Phytochemical, Antimicrobial, and Toxicological Evaluation of Traditional Herbs Used to Treat Sore Throat.

The in vitro antibacterial activities of 29 traditional medicinal plants used in respiratory ailments were assessed on multidrug resistant Gram-positive and Gram-negative bacteria isolated from the sore throat patients and two reference strains. The methanolic, n-hexane, and aqueous extracts were screened by the agar well diffusion assay. Bioactive fractions of effective extracts were identified on TLC coupled with bioautography, while their toxicity was determined using haemolytic assay against human erythrocytes. Qualitative and quantitative phytochemical analysis of effective extracts was also performed. Methanolic extract of 18 plants showed antimicrobial activity against test strains. Adhatoda vasica (ZI = 17-21 mm, MIC: 7.12-62.5 µg/mL), Althaea officinalis (ZI = 16-20 mm, MIC: 15.62-31.25 µg/mL), Cordia latifolia (ZI = 16-20 mm, MIC: 12.62-62.5 µg/mL), Origanum vulgare (ZI = 20-22 mm, MIC: 3-15.62 µg/mL), Thymus vulgaris (ZI = 21-25 mm, MIC: 7.81-31.25 µg/mL), and Ziziphus jujuba (ZI = 14-20 mm, MIC: 7.81-31.25 µg/mL) showed significant antibacterial activity. Alkaloid fractions of Adhatoda vasica, Cordia latifolia, and Origanum vulgare and flavonoid fraction of the Althaea officinalis, Origanum vulgare, Thymus Vulgaris, and Ziziphus jujuba exhibited antimicrobial activity. Effective plant extracts show 0.93-0.7% erythrocyte haemolysis. The results obtained from this study provide a scientific rationale for the traditional use of these herbs and laid the basis for future studies to explore novel antimicrobial compounds.

Dermatoprotective effects of some plant extracts (genus Ficus) against experimentally induced toxicological insults in rabbits.

AIM: Present study was conducted to evaluate the dermatoprotective effects of plant extracts (Ficus religiosa, Ficus benghalensis, and Ficus racemosa) against known irritants such as sodium dodecyl sulfate (SDS), atrazine, and petrol. METHODS: The study was conducted in adult male rabbits. Ethanol extracts of plants were obtained through Soxhlet. All irritants and Ficus extracts were topically applied to the backs of rabbits daily for 4 days, while pure ethanol served as control. Skin was examined after 24, 48, and 96 h for erythema. Skin biopsies were taken on 5th day for microscopic examination. RESULTS: Erythema produced by irritants reduced significantly with the simultaneous application of Ficus extracts. The mean ± SEM epidermal thickness (micrometer) with SDS was 45.40 ± 1.89, F. religiosa + SDS was 18.60 ± 0.51, F. benghalensis + SDS was 18.40 ± 0.25, F. racemosa + SDS was 18.80 ± 0.37, and mixture of three Ficus species + SDS was 16.80 ± 0.37. Similar findings were revealed after using plant extracts with atrazine and petrol. The mean ± SEM epidermal layer count for SDS was 3.60 ± 0.25, atrazine was 3.40 ± 0.25, petrol was 3.40 ± 0.25, and ethanol (control) was 1.00 ± 0.20. This count reduced to 1.20 ± 0.20 for three Ficus species + SDS, 1.40 ± 0.25 for Ficus species + atrazine, and 1.40 ± 0.25 for Ficus species + petrol. CONCLUSION: Ficus species demonstrated the potential to block the dermatotoxic effects of topical irritants and could be used successfully to prevent skin toxicity.