Md. Akhlaquer Rahman

Current approaches toward production of secondary plant metabolites

Plants are the tremendous source for the discovery of new products with medicinal importance in drug development. Today several distinct chemicals derived from plants are important drugs, which are currently used in one or more countries in the world. Secondary metabolites are economically important as drugs, flavor and fragrances, dye and pigments, pesticides, and food additives. Many of the drugs sold today are simple synthetic modifications or copies of the naturally obtained substances. The evolving commercial importance of secondary metabolites has in recent years resulted in a great interest in secondary metabolism, particularly in the possibility of altering the production of bioactive plant metabolites by means of tissue culture technology. Plant cell and tissue culture technologies can be established routinely under sterile conditions from explants, such as plant leaves, stems, roots, and meristems for both the ways for multiplication and extraction of secondary metabolites. In vitro production of secondary metabolite in plant cell suspension cultures has been reported from various medicinal plants, and bioreactors are the key step for their commercial production. Based on this lime light, the present review is aimed to cover phytotherapeutic application and recent advancement for the production of some important plant pharmaceuticals.

Role of excipients in successful development of self-emulsifying/microemulsifying drug delivery system (SEDDS/SMEDDS)

The oral delivery of hydrophobic drug presents a major challenge because of the low aqueous solubility of such compounds. Self-emulsifying/microemulsifying drug delivery system (SEDDS/SMEDDS), which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. The efficiency of oral absorption of said drug from such type of formulation depends on many formulation-related parameters, such as surfactant concentration, oil/surfactant ratio, polarity of the emulsion, droplet size and charge, all of which in essence determine the self-emulsification ability. Thus, only very specific pharmaceutical excipient combinations will lead to efficient self-emulsifying systems. With the growing interest in this field, there is an increasing need for guidelines in excipient selection to obtain effective delivery system with improved bioavailability. The aim of this review is to present the recent approaches in selecting the most appropriate lipid system(s); methods for its characterization and role of various excipients for improved delivery of dosage form.

Validation of the method for the simultaneous estimation of bioactive marker gallic acid and quercetin in Abutilon indicum by HPTLC

Abstract Objective To establish and validate an simultaneous estimation of the two biomarker compounds gallic acid (GA) and quercetin (QE) from methanolic extract of Abutilon indicum (AI). Methods Chromatography was performed on aluminium foil-backed silica gel 60 F254 HPTLC plates with the binary mobile phase toluene-ethyl acetate-formic acid (5:4:1, v/v/v). Ultraviolet detection was performed densitometrically at the maximum absorbance wavelength, 270nm. The method was validated for precision, recovery, robustness, specificity, and detection and quantification limits, in accordance with ICH guidelines. Results The system was found to give compact spots for GA and QE (Rf value of 0.31 and 0.50, respectively). The limit of detection (23 and 41 ng band-1) limit of quantification (69 and 123 ng band-1), recovery (99.4–99.9 and 98.7–99.4%), and precision (≤1.98 and 1.97) were satisfactory for gallic acid and quercetin respectively. Linearity range for GA and QE were 100-1000 (r 2 = 0.9991) and 150–900 ng band-1 (r 2 = 0.9956) and the contents estimated as 0.69% ± 0.01% and 0.57% ± 0.01% w/w respectively. Conclusions This simple, precise and accurate method gave good resolution from other constituents present in the extract. The method has been successfully applied in the analysis and routine quality control of herbal material and formulations containing AI.

Agricultural, Pharmaceutical, and Therapeutic Interior of Catharanthus roseus (L.) G. Don

Catharanthus roseus (C. roseus) (L.) G. Don known as Madagascar periwinkle (MP) is a popular ornamental plant found in gardens and homes across the world. C. roseus (L.) G. Don has been widely distributed for long enough and gained popularity as diverse application in medicinal uses for a variety of purposes such as antimicrobial, antioxidant, anthelmintic, antifeedant, antisterility, antidiarrheal, and antidiabetic effect and have been used in the treatment of leukemia, Hodgkin’s disease, malignant lymphomas, neuroblastoma, Wilms tumor, Kaposi’s sarcoma, and mycosis fungoides to improve cerebral blood flow and treat high blood pressure. The pharmacology of the plant was found to be associated mostly especially with the alkaloids that occupies almost all parts of the plant. C. roseus (L.) G. Don is a legendary medicinal plant mostly because of possessing two invaluable antitumor terpenoid indole alkaloids (TIAs), vincristine and vinblastine. The ethnobotanical significance of C. roseus (L.) G. Don is exemplified by its international usage as a traditional remedy for abundant ailments and not only for cancer. TIAs are present only in micro quantities in the plant and are highly poisonous per se rendering a challenge for researchers to increase yield and reduce toxicity. Good agronomic practices ensure generous propagation of healthy plants that serve as a source of bioactive compounds and multitudinous horticultural applications. In this chapter, an attempt has been made to summarize the agricultural, pharmaceutical, and pharmacological applications in a precise way to help the scientists and learners to understand the basic values of the plant.

Development and in vitro/in vivo evaluation of artemether and lumefantrine co-loaded nanoliposomes for parenteral delivery

Abstract Combination therapy of artemether (ART) and lumefantrine (LUM) is well-established for the treatment of uncomplicated malaria worldwide. Nanoliposomes (NLs) encapsulating both drugs were prepared and freeze-dried. The lyophilized nanoliposomes exhibited high entrapment efficiency of artemether (66.18%), relatively low entrapment efficiency of lumefantrine (53.46%), low average size diameter (125.3 nm) and found to be stable at 4 °C for 60 days without significant change in mean particle diameter and drug entrapment efficiencies. In vitro drug release study has shown initial burst effect and then sustained release pattern over a time period of 30 h. In vivo toxicity study was examined by liver and kidney function test as well as histopathological examination. Nanoliposomes showed lower hemolytic potential (∼10%) compared to all the components when studied individually. There was no significant change (p > 0.05) in biochemical parametes between control and treated group of animals. Pharmacokinetic data of ART + LUM NLs showed higher the area under the plasma concentration–time curve (AUC) values and prolonged residence time of drug in the blood circulation compared with ART + LUM solution. The tissue distribution demonstrated high uptake of ART + LUM-NLs in RES organs particularly in liver and spleen. Biocompatibility was confirmed by hepato- and nephrotoxicity analysis showed no sign of fibrosis, fatty infiltration, centrilobular necrosis and lymphocyte infiltration confirmed the suitability of developed formulation for treatment of malaria.

HPTLC METHOD FOR ANALYSIS OF SERTRALINE IN PURE BULK DRUG AND LIPIDIC NANO DELIVERY SYSTEM: A STRESS DEGRADATION STUDIES

A sensitive, selective, precise, and stability-indicating, high-performance, thin-layer chromatographic (HPTLC) method for analysis of sertraline, both as a bulk drug and in house formulation, was developed and validated. The method employed thin-layer chromatographic (TLC) aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of Toulene/Ethyl acetate/Ammonia (1:5:0.1, v/v) as a mobile phase. The densitometric analysis were carried out at 273 nm using Camag TLC scanner which generated compact spots for SRT (R f = 0.70 ± 0.02). The linear regression data for the calibration plots showed good linear relationship with r2 = 0.998 in the concentration range of 25–2000 ng spot−1. Sertraline was subjected to acid and alkali hydrolysis, oxidation, photodegradation, and dry heat treatment. Also, the degraded products were well separated from the pure drug. The method was validated for precision, accuracy, ruggedness, and recovery. As the method could effectively separate the drug from its degradation products, it can be employed as a stability indicating one. Moreover, the proposed HPTLC method was utilized to investigate the kinetics of acid and base degradation process.

Solvent Extraction and Gas Chromatography–Mass Spectrometry Analysis of Annona squamosa L. Seeds for Determination of Bioactives, Fatty Acid/Fatty Oil Composition, and Antioxidant Activity

ABSTRACT The yield and fatty oil components of the seed kernels of Annona squamosa L. (Family: Annonaceae) were determined by solvent extraction method and gas chromatography–mass spectrometry (GC-MS). Seeds were extracted with ethanol and further fractionated with n-hexane. The free radical–scavenging activities of both ethanolic and n-hexane fraction against 1, 1-diphenyl-2-picrylhydrazyl (DPPH) were determined by UV spectrophotometer at 517 nm. Phytochemical screening revealed the presence of numerous bioactive compounds including steroids, flavonoids, terpenoids, fatty acids, and different types of ester compounds. The prevailing compounds found in ethanolic fraction were n-hexadecanoic acid (10.08%), heptadecene-(8)-carbonic acid-(1) (29.68%), octadecanoic acid (3.61%), 9-octadecenoic acid (Z)-2,3-dihydroxypropyl ester (5.14%), ergost-5-en-3-ol (3.68%), stigmasta-5,22-dien-3-ol (5.93%), and y-sitosterol (8.25%). Compounds found in n-hexane fraction were mainly n-hexadecanoic acid (14.42%), 9,12-octadecadienoic acid (2.87%), cis-vaccenic acid (10.39%), 9-octadecenoic acid (7.03%), hexadecanoic acid, 2-hydroxy-1-(hydroxymethyl) ethyl ester (4%), 9-octadecenoic acid (Z)-, 2,3-dihydroxypropyl ester (13.33%), ergost-5-en-3-ol (4.04%), stigmasta-5,22-dien-3-ol, (3.beta.,22e) (6.07%), and y-sitosterol (10.87%). The crude fatty oil was converted into methyl esters and analyzed by GC-MS. Eleven compounds constituting 99.9% of the oil were identified. The presence of saturated and unsaturated fatty acids in ethanolic and n-hexane fraction of A. squamosa seed extract justify the use of this plant to treat many ailments in folk and herbal medicine. Both the fractions have shown significant antioxidant activity. The presence of phenolic compounds and unsaturated fatty acids are reported as possible contributors for antioxidant activity of seed extract.

The Role of Tamarix gallica Leaves Extract in Liver Injury Induced by Rifampicin Plus Isoniazid in Sprague Dawley Rats

ABSTRACT The Tamarix gallica leaves extract (TGLE) was investigated for hepatoprotective potential against rifampicin (RIF) plus isoniazid (INH)–induced liver injury in Sprague Dawley (SD) rats. All the rats of groups III and IV received 100 and 200 mg/kg body wt, respectively, of the suspension of TGLE while group V received silymarin 100 mg/kg body wt orally. After 10 min, they, along with group II, received INH plus RIF each day (50 mg/kg body wt, by mouth (PO) each) for 28 days. Group I received 10 ml/kg body wt, PO of vehicle, i.e., 1% aqueous carboxymethyl cellulose (1% CMC) throughout the study. At the end of the experiment, blood was obtained through the retro-orbital plexus under light anesthesia and the serum was separated from the sacrificed animals. A small portion of isolated liver tissue was fixed in 10% formaldehyde for histopathological examinations. The levels of elevated serum bilirubin (p > .05–p < .05), alanine transaminase (p > .05–p < .01), aspartate transaminase (p > .05–p < .01), alkaline phosphatase (p < .05–p < .01), lactate dehydrogenase (p < .05–p < .01), and cholesterol (p > .05–p < .01) decreased while the levels of decreased total protein (p > .05–p < .05) and albumin (p < .05–p < .05) increased in TGLE-treated groups III and IV as compared to group II, and the serum marker enzyme levels were toward normal, indicating protection against liver injury. It was well supported with histopathological results. Thus, Tamarix gallica leaves extract possesses promising hepatoprotective activity against RIF plus INH-induced liver injury in experimental rats.