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Background Objective of present research work is to develop and validate cost-effective analytical tool for determination of camptothecin (CPT) and determine its anticancer potential against prostate cancer LNCaP cell lines. Structural elucidation has been performed by mass spectrometry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, and MTT assay utilized for in vitro cytotoxicity where spectrometric method was used for estimation of camptothecin. Results Mass spectra showed peak at 349.2 which matches to standard molecular weight of camptothecin. FTIR and NMR spectra conformed functional moieties and structure of isolated camptothecin which was nearly equal to values mentioned in standard structure of camptothecin. IC50 values of CPT against LNCaP cell lines was found to be 3.561 μg/ml. Lambda max of CPT was found to be at 225 nm and calibration curve found to be linear over the concentration range from 2 to 70 μg/ml of camptothecin. Developed method was found to be linear, accurate, and precise. LOD and LOQ were found to be 0.0524 μg/ml and 0.1614 μg/ml, respectively. Developed method has % relative standard deviation less than one which is reproducible hence % recovery was found to be 99.80%. Conclusions FTIR, NMR, and mass spectrometry results conforms isolated compound was camptothecin; cytotoxicity study proves it has strong potential in treatment of prostate carcinoma as competent alternative to chemotherapy in the form of herbal medicine and the developed UV method proves to be valid, sensitive, and applicable for rapid, accurate, precise, and economical determination of camptothecin.

The present investigation deals with the pazopanib-loaded solid lipid nanoparticles (Pazo-SLNs) and their in-vitro and in-vivo assessments. Quality by design approach employing the Plackett-Burman and central composite design was used to identify the formulation variables, including drug/lipid ratio, organic/aqueous phase ratio, and surfactant concentration with a significant impact on the process and to fabricate a safe and efficacious novel oral dosage form of pazopanib. Particle size, drug loading, entrapment efficiency, and zeta potential of optimal Pazo-SLNs formulation were 210.03 ± 7.68 nm, 13.35 ± 0.95 %, 79.05 ± 2.55 % and -18.29 ± 1.89 mV (n = 3) respectively. FTIR study affirmed the absence of incompatibilities between the drug and the excipients. DSC and XRD measurements substantiated the amorphous form of pazopanib entrapped within the SLNs. Pazo-SLNs demonstrated high cellular uptake, showed substantial cytotoxicity to A-549 lung cancer cells due to apoptotic mode and inhibited tyrosine kinase in-vitro. Pazo-SLNs were found to be stable for three months. SLNs greatly ameliorated the pharmacokinetic behavior and bioavailability (9.5 folds) of pazopanib with a sustained-release pattern (92.67 ± 4.68 % within 24 h). A biodistribution study corroborated the lung targeting potential of Pazo-SLNs. Thus, SLNs could potentially boost the oral route efficacy of pazopanib against cancer cells.

In this investigation, the fabrication of capsaicin loaded self nano emulsifying drug delivery system (SNEDDS) was attempted to improve the effectiveness of capsaicin through the oral route. A pseudo-ternary phase diagram was constructed at different km values (1:1, 2:1,3:1). Nine liquid formulations (L-CAP-1 to L-CAP-9) were prepared at km = 3, evaluatedconverted to solid free-flowing granules using neusilin® US2. L-CAP-3 comprising of 15% isopropyl myristate, 33.75% Labrafil,11.25% ethanol exhibited higher % transmittance (98.90 ± 1.24%)lower self-emulsification time (18.19 ± 0.46 s). FT-IR spectra showed no incompatibility whereas virtual analysis confirmed hydrogen bond interaction between amino hydrogen in the capsaicinoxygen of the neusilin. DSCXRD study revealed the amorphizationmolecular dispersion of capsaicin in S-SNEDDS. TEM analysis confirmed the nano-sized spherical globules. Within 15 min, L-SNEDDS, S-SNEDDS,pure capsaicin showed 87.36 ± 3.25%, 85.19 ± 4.87%,16.61 ± 3.64% drug release respectively. S-CAP-3 significantly (P 0.001) inhibited the proliferation of HT-29 colorectal cancer cells than capsaicin. Apoptosis assay involving Annexin V/PI staining for S-CAP-3 treated cells demonstrated a significant (P 0.001) apoptotic rate. Remarkably, 3.6 fold increase in bioavailability was observed after oral administration of capsaicin-SNEDDS than plain capsaicin.

Objectives Mycobacterium tuberculosis is the causative organism of tuberculosis, which is the most lethal disease after cancer in the current decade. The development of multidrug and broadly drug-resistant strains is making the problem of tuberculosis more and more critical. In the last 40 years, only one molecule has been added to the treatment regimen. Generally, drug design and development programs target proteins whose function is known to be essential to the bacterial cell. M. tuberculosis possesses specialized protein export systems like the SecA2 export pathway and ESX pathways. Materials and methods In the present communication, rational development of an antimycobacterial agent's targeting protein export system was carried out by integrating pocket modeling and virtual analysis. Results The 23 identified potential lead compounds were synthesized, characterized by physicochemical and spectroscopic methods like infrared and nuclear magnetic resonance spectroscopy, and further screened for antimycobacterial activity using isoniazid as standard. All the designed compounds showed profound antimycobacterial activity. Conclusion We found that Q30, M9, M26, U8, and R26 molecules had significant desirable biological activity and specific interactions with Sec of mycobacteria. Further optimization of these leads is necessary for the development of potential antimycobacterial drug candidates with fewer side effects.

The research work was aimed to formulate and evaluate sustained release tablet of guanfacine hydrochloride which deliver drug for 24 hours. In this developed formulations pH dependent and pH independent polymers such as hydroxyl propyl methyl cellulose and eudragit L 100-55 was utilized to prepare matrix tablet. Guanfacine hydrochloride extended release tablet reduces the dosage frequency, enhance patient compliance and maintain the therapeutic effect of the drug throughout the day. The dosage regimen of guanfacine hydrochloride is 4 mg at every 6 hours. The concentration of guanfacine in plasma is fluctuating. Hence, to control the plasma fluctuation and to avoid toxicity problem, guanfacine hydrochloride was chosen as a drug with an aim to develop an extende release system for 20 to 24 hours. The design of system was based on the use of pH dependent polymer, pH independent polymer, along with microenvironment modifiers such as organic acid (fumaric acid) were used in the formulation. The effect of different formulation variables, namely, amount of polymer concentration, different grade of polymer and effect of different method on release profile were studied. Drug-excipients compatibility was studied by FTIR. Before compression, the granules were evaluated for precompression parameters such as bulk density, tapped density, angle of repose, compressibility index and Hausner’s ratio. After compression, evaluation tests of tablets such as general appearance, hardness, thickness, weight variation, friability, content uniformity, in vitro release studies and stability studies were performed. Stability study of formulation F9 revealed there was no significant change in physical and chemical properties of drug stored at 40°C/75 % RH, 30°C/65 % RH, 25°C/60 % RH. The study indicates that guanfacine hydrochloride extended release tablet was successfully developed.

Aim of the present investigation was to assess and compare the in-vitro and in-vivo cancer targeting propensity of DPPE–FA–DOX Micelles and free DOX in tumor bearing BALB/c mice. The DOX was conjugated with 1, 2-Dihexadecanoyl-sn-glycero-3-phosphoethanolamin (DPPE) and folic acid using Di-cyclohexyl-carbodiimide, confirmed by Fourier transform infrared spectroscopy (FTIR) and proton NMR. DPPE–FA–DOX micelles were prepared using thin film method and evaluated for zeta potential, particle size, surface morphology, in- vitro drug release study etc. In-vitro anticancer activity and apoptosis assay was evaluated in breast cancer (MCF-7) cells using MTT assay and flow cytometer respectively. In-vivo biodistribution and toxicity assessment were evaluated in rats whereas antitumor activity in tumor bearing BALB/c mice. Prepared micelles were spherical with size and zeta potential of 295.6 + 84.4 nm and 0.8 ± 0.24 mV respectively. Apoptosis assay for DPPE–FA–DOX micelles treated cells using Annexin V/PI staining demonstrated 56.2% apoptotic cells. Remarkably, DPPE–FA–DOX micelles improved DOX bioavailability by 7 fold and diminished plasma elimination with no sign of tissue toxicity compared to free DOX. In-vivo biodistribution studies revealed that micelles facilitated higher accumulation of DOX in tumor than free DOX. DPPE–FA–DOX micelles treated mice survived for 62 days than Free DOX (40 days), revealed by Kaplan-Meier survival curve analysis. Histopathological examination of liver, kidney and heart tissues of micelles treated rat’s corroborated reduced systemic toxicity than free DOX. Conclusively, DPPE–FA–DOX micelles could potentially facilitate the targeted delivery of DOX to tumors.

The study was initiated with the intent to synthesize acrylamide grafted neem gum polymer (AAm-g-NG), and screen its drug release retardation ability both in vitro and in vivo. Different batches (NGP-1 to NGP-9) of tablet formulation were prepared by varying polymer concentration using propranolol HCl and compared with HPMC K100 M and marketed SR tablets. FTIR study proved the grafting phenomenon and showed no incompatibility between AAm-g-NG and propranolol HCl. AAm-g-NG showed significant swelling and water retention capacity than NG. AAm-g-NG was found to be biodegradable and exhibited no toxicity to Artemia salina. After 12 h, NGP-6 showed non-significant (p > 0.05; f2= ∼ 90) percent drug release (80.52 ± 3.41%) compare to marketed formulation (79.65 ± 4.08%). Significant swelling of the matrix caused slower diffusion of the drug. NGP-6 and marketed formulation in rabbits showed the non-significant difference between Cmax and Tmax, hence NGP-6 meets the requirement of sustained-release tablets.

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12451 International Current Pharmaceutical Journal 2012, 1(12): 414-419

Objective of the present study is to develop simple, easily accessible, economic, newer conductometric method of estimation for Telmisartan. Telmisartan is weak acid due to presence of acidic functional group which can be estimated by conductometric method in alcoholic media. The developed method was validated according to ICH guidelines for parameters like accuracy, precision, specificity, ruggedness, robustness and percentage recovery. Results: The Relative Standard Deviation was 0.701677; recovery was 98-100%. Tablet formulations were used as sample for estimation and the results are found to be well within the specified limit. Conclusion: Therefore developed method can used for estimation of Telmisatan in pure or in formulations. Key words: Conductometry, Telmisartan, Estimation, Weak acid.

A simple, specific and accurate reverse phase liquid chromatographic method was developed for determination of Azilsartan in its tablet dosage form as well as from biological fluid like plasma. The determination was carried out on ODS Hypersil C18 column (4.6 mm x 250 mm 5µm) column using a mobile phase of acetonitrile: water (pH 4) [60: 40 %v/v]. The flow rate was 1 mL/min with detection at 249 nm. The linearity response of the HPLC system for Azilsartan was obtained over the range 1-64 µg/mL. Ambroxol (25µg/mL) was used as internal standard. Retention time for Azilsartan and ambroxol were found to be 3.74 and 1.84 minutes respectively. The correlation co-efficient (R2 value) for Azilsartan was found to be 0.992. The proposed method was successfully used for quantification of Azilsartan in Azilva tablets and plasma. The method was validated as per ICH Q2B (Analytical) and USFDA (Bio-analytical) guidelines. The results of analysis have been validated statistically and by recovery studies. The method is found useful for quantification of Azilsartan in marketed formulations as well as from biological fluids and can be applied for quantification of Azilsartan in preclinical and clinical studies.

Herbal cosmetics are gaining popularity as nowadays most women prefer natural products over chemicals for their personal care and to enhance their beauty. Compared to other beauty products, natural cosmetics are safe to use. Synthetic colouring agents may cause allergic reactions and were found to be carcinogenic. Aim of present study was to formulate and evaluate herbal lipstick using lycopene extracted from Solanum lycopersicum L. as a colouring agent. Along with lycopene different natural ingredients such as bees wax, carnuba wax, white soft paraffin, castor oil, strawberry essence and lemon juice were used to formulate herbal lipstick. Prepared herbal lipstick were evaluated for different evaluation test such as colour, texture, pH, melting point, breaking point, softening point, surface anomalies, ageing and perfume stability and also compared with marketed standard formulation. Results showed that, different evaluation parameters of prepared herbal lipstick were resembled with standard values and with marketed formulation. Study concluded that, lycopene extracted from Solanum lycopersicum L. may be better option for synthetic colouring agent.

Pellets are small free flowing; spherical particulates manufactured by the agglomeration of fine powder or granules. Different types of techniques used to produce pellets are referred to as pelletization techniques. In relation to pharmaceuticals, pellets offer high degree of flexibility in design and development of oral dosage form. They offer desired dose strength, can be blended to deliver incompatible bioactive agents and can be blended to provide different release profiles. The most commonly use pelletization processes are Extrusion spheronization, Hot melt extrusion, Solution or suspension layering, Powder layering, High shear pelletization, Freeze pelletization, Cryopelletization, Crystallo-co-agglomeration, Wet spherical agglomeration, Spherical crystallization etc. In present review we will be explaining widely used pelletization techniques especially are Extrusion Spheronization and Hot Melt Extrusion in detail with methods and applications in pharmaceutical industries because these techniques represent an efficient pathway for novel drug delivery system today.