NANO-BASED THERAPY FOR TREATMENT OF SKIN CARCINOMA

Skin carcinoma is a frequently occurring cancer caused due to ultra violet rays of the Sun. It starts from normal skin cells but later on transforms into cells which undergo uncontrolled mitosis. Skin cancer is not as deadly as other cancers and has no metastasis and is not life threatening. Conventional chemotherapy has in general failed to treat skin cancer due to non specific targeting, which is accompanied by several side effects. Novel therapeutic approach based on nanotechnology have emerged as the best alternative for skin cancer treatment. We presented current scenario of nano based particulate drug carrier approaches for effective therapy for skin carcinoma by reducing side effects. This approach also reduces frequency of administration and improves patient compliance. Nanotechnology has emerged as the best alternative for conventional therapy for the effective treatment of skin cancer. Nanoparticles can specifically target skin carcinoma and are able to sustain drug release and reduce side effects to a greater extent.

VALIDATED STABILITY INDICATING SPECTROSCOPIC METHOD FOR ESTIMATION OF DEGRADATION BEHAVIOUR OF VALSARTAN AND HYDROCHLOROTHIAZIDE IN TABLET FORMULATION

A simple, accurate and precise UV spectrometric method has been developed for the simultaneous determination of valsartan and hydrochlorothiazide in tablet dosage form. Spectra of valsartan and hydrochlorothiazide in methanol and water (50:50 V/V) show λ max at 250.0 nm and 271.4 nm, respectively. Valsartan and hydrochlorothiazide are subjected to various stress conditions like acid, alkali, thermal and photolytic degradation. Beer’s law was obeyed in concentration range of 4- 24 µg mL-1 for valsartan and 0.5-3 µg mL-1 for hydrochlorothiazide at their respective wavelengths. The proposed method was successfully applied to tablet dosage form for determination of both drugs. The percentage recovery of valsartan and hydrochlorothiazide were found to be 100.19 % and 99.51 %, respectively. A novel accurate and precise stability indicating spectroscopic method has been developed for estimation of valsartan and hydrochlorothiazide.

EXTRACTION, ISOLATION, CHEMICAL IDENTIFICATION AND IN VITRO UROLITHIATIC ACTIVITY OF PIPERINE FROM PIPER NIGRUM

Piper nigrum is belongs to the family Piperaceae. The aim of the present study was to extract, isolate and investigate in vitro urolithiatic activity of alkaloid (piperine) from black pepper and identification by chemical reagents. In vitro urolithiatic evaluation of piperine was performed by percentage dissolution and turbidity methods. Calcium oxalate crystals were synthetically prepared and packed in a semipermeable membrane in both methods. Results were compared statistically and it showed significant P​

PREPARATION AND EVALUATION OF BB CONCEALER CREAM CONTAINING NEEM OIL FOR ACNE TREATMENT

Acne vulgaris is a chronic dermatological inflammatory disease with symptoms like redness, comedones and blemishes appearing on face and neck. Propionobacterium acnes plays an important role in this disease. Neem oil, an ayurvedic, anti-bacterial medicine is non-comedogenic. Concealer is a type of cosmetic used to mask and camouflage blemishes and imperfections visible on skin and are available as liquid, balm, cream and stick. BB creams in cosmetics is termed as “beauty balm, blemish base, blemish balm” designed to serve as foundation, moisturizer and sunscreen all at once. The current study was to develop an aesthetic BB cream combining an anti-acne activity with concealing effect. Concentrations of upto 25 %w/w neem oil was prepared and evaluated for appearance, texture, pH, spreadability, antibacterial properties and in vitro release studies. All the formulations confirmed activity against P. acnes. Prolonged activity of neem oil observed at the end of 6 h as demonstrated in vitro

QSAR STUDIES ON HUMAN CARBONIC ANHYDRASE II INHIBITORS

Carbonic anhydrase II is one of the forms of human α carbonic anhydrases which are ubiquitous metalloenzymes that catalyze inter-conversion of carbon dioxide and water to bicarbonate and proton, overexpression of which leads to disorders such as glaucoma. 2D and 3D Quantitative Structure Activity Relationship studies were carried out on previously synthesized series of sulfanilamide derivatives by VLife MDS software using stepwise variable, multi-linear regression and k-nearest neighbor molecular field analysis methods. 2D-QSAR model depicts contribution of halogens (such as chlorine and fluorine), methylene and oxygen atoms to inhibition of human carbonic anhydrases II activity. Using k-nearest neighbor molecular field analysis method two 3D-QSAR models (model A and B) were generated from which model A was found to be the best validated model with q2 (0.9494), pred_r2 (0.7367) and q2 _ se (0.2037). It displayed the fact that the inhibitory action of sulfanilamide derivatives against human carbonic anhydrases II is influenced by hydrophobicity and electro positivity.

EVALUATION OF IN VITRO ANTIOXIDANT AND IN VIVO HEPATOPROTECTIVE ACTIVITY OF BAUHINIA VARIEGATA ROOT ETHANOLIC EXTRACT AGAINST CCL4 INDUCED LIVER INJURY IN RATS

Plant derived herbal formulations and remedies provide an effective means for the treatment of various types of disease that are dogmatic and incurable in other types of systems of medicines, but it is essential to explore and establish the scientific basis for therapeutic action of herbal plant medicines. Bauhinia variegata root ethanolic extract was studied for the hepatoprotective activity against CCl4 induced liver injury in rats. For estimation of hepatoprotective role of B. variegata, total bilirubin count, serum enzymes level and finally histopathological study of liver were performed. This extract’s DPPH radical scavenging potential was also studied. The ethanolic extract of B. variegata root administered orally to animal showed significant depletion in CCL4 induced increased level of SGPT, SGOT, ALP and total bilirubin concentration. Significantly (p<0.05), hepatotoxicity is reversed by treatment with Liv 52 syrup also. For initiation of biochemical analysis, the histopathological studies are provided supportive evidence. This extract also showed better activity in quenching DPPH radical. The ethanolic extract of B. variegata root shows antioxidant property by preventing the formation of trichloromethyl peroxy radicals, and thus reduce tissue damage, which is examined and confirmed by the histopathological studies. Therefore, the hepatoprotective activity of ethanolic extract of B. variegata root may be due to its antioxidant potential. Previously studies have reported that plants containing flavonoids possess antioxidant properties. The antioxidant and hepatoprotective properties of the test plant may be attributed to the presence flavonoids. B. variegata root ethanolic extract is shown to have hepatoprotective and antioxidant action.

EXCITING TIMES AHEAD FOR THE INDIAN PHARMA INDUSTRY

Dear Reader, Coinciding with the 60th Anniversary of IDMA, a true and vibrant transition phase is commencing for your association, its publications and allied activities. Dr. Viranchi Shah, the young and energetic Hon. President from “Vibrant Gujarat” is taking over the reigns of IDMA, with an equally young team of Executive committee members. We are confident that IDMA’s flag will fly high globally, all the more, in the coming years. It is time that the young (and the long-experienced ones too) get ready for the new integrated and synergised challenges of the 2020’s and 2030’s to keep pace with the clarion call for intense pharma research and innovation to keep pace with the west and the rest.

DERIVITISATION OF PREGABALIN FOR SIMULTANEOUS ESTIMATION WITH METHYLCOBALAMINE USING ULTRAVIOLET SPECTROSCOPY

Accurate, sensitive, and economical procedures for simultaneous estimation of pregabalin and methylcobalamine in tablet dosage form have been developed. The method employed is simultaneous equation method. This method employs the formation and solving of simultaneous equation using 528 nm and 568 nm as the two wavelengths for forming equation. Drugs obey Beer’s law in the concentration range 10-50 µg mL-1 for pregabalin and 10-50 µg mL-1 for methylcobalamine. The proposed spectrophotometric method was validated and successfully applied for the assay of both drug combinations in several laboratory prepared mixtures and commercial tablets

STABILITY INDICATING RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF SIMETHICONE, DOMPERIDONE, MAGALDRATE AND SODIUM ALGINATE: APPLICATION TO SYRUP FORMULATION

A rapid and validated stability indicating RP-HPLC method using isocratic elution and coupled with photodiode array detection was developed for quantifying the content of simethicone, domperidone, magaldrate and sodium alginate in bulk and syrup formulation. The best mobile phase used in this study consisted of 0.1 % orthophosphoric acid/acetonitrile (50/50, V/V) with a flow rate of 0.7 mL min-1. Under optimized conditions used in this study, selected drugs were eluted at 3.301 min (simethicone), 4.293 min (domperidone), 5.220 min (magaldrate) and 6.149 min (sodium alginate) within 12 min run time without any interfering excipients. Peak areas and selected drug content demonstrated excellent linearity (simethicone – 5 to 30 µg mL-1; domiperidone – 2.5 to 15 µg mL-1; magaldrate – 120 to 720 µg mL-1; sodium alginate – 25 to 150 µg mL-1). Percent recovery, which represents accuracy, was 99.12–100.18 % for simethicone, 99.59-100.52 % for domperidone, 99.23-100.25 % for magaldrate and 99.57-100.02 % for sodium alginate. Percent relative standard deviation, which represents precision, was observed in the range of 0.078-0.983 % (simethicone), 0.528-0.861 % (domperidone), 0.278-1.069 % (magaldrate), 0.316-0.572 % (sodium alginate). The developed method displayed favourable accuracy and recovery and was suitable for determining the content of simethicone, domperidone, magaldrate and sodium alginate combination in syrup formulations.

FORMULATION DEVELOPMENT OF ORLISTAT NANOCRYSTALS: IN VITRO CHARACTERIZATION AND IN VIVO STUDIES

Poor solubility of orlistat limits its luminal concentration and hence needs to be administered in higher doses, leading to drug related side effects. The aim of the present research was to investigate nanocrystallization approach to increase the solubility of orlistat using melt extrusion and high-pressure homogenization (HPH) methods. The effect of factors like type and amount of polymer, homogenization pressure and time, and number of cycles on orlistat solubility was investigated. A ~10-fold increase in the solubility of orlistat was attained using OPo11N with a subsequent increase in the dissolution rate of the drug. Poloxamer 188-orlistat nanocrystals (OPo11N) as compared to pure orlistat led to a decrease in T90%(20 mins for OPo11N and 51 mins for marketed sample). In vivo studies in female Sprague Dawley (SD) rats showed that post one month of oral administration the total cholesterol and low-density lipoproteins of female SD rats remained unchanged compared to the control group. The triglycerides content and high-density lipoproteins levels were significantly increased with increase in the treatment time i.e. 12 weeks compared to the group treated with pure orlistat drug. In conclusion, the NC approach could serve as an effective formulation strategy for solubility enhancement of orlistat.