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Ayurvedic lipid based rasayans - A perspective on the preparation and pharmacological significance of lipids on the bioavailability of phytoconstituents.

ABSTRACT: For thousands of years, lipid based Ayurvedic formulations have been made in India, and the craft has survived down the millennia up to the present time. Some of these deliciously potent phytonutrient preparations are very popular and have sustained the test of time pertaining to their efficacy. Recent researches on the role of phytonutrients in promoting cardio-pulmonary, brain and immune health substantially buttress the philosophy underlying the use of lipids in preparing these emulsions, since a large number of these bioactives are lipophilic. Being lipoidic, they are absorbed through the lacteals in the small intestine, and are then transported through the thoracic duct directly to the heart, bypassing the liver. The formulations utilizing ghee (clarified butter) or sesame oil as the carrier lipid, either while frying the myrobalams or as Anupana (adjuvant), have special significance in modulating bodily immunity, since the immune system is housed in lymphatics which are lipid rich. Amla and lipid based Ayurvedic rasayans (rejuvenating formulations) are a popular and highly palatable group of phytonutraceutical preparations. This group of polyherbal adaptogenic formulations is classified separately from other formulations in Ayurvedic therapeutics. Several of these health-promoting rasayans are suitable to be consumed by all age-groups in the recommended season and dose. Current research on endothelial and immune cell receptor mediated uptake of lipoidic molecules, together with the knowledge of lipid absorption pathways, lends credence to the usefulness of rasayans in targeting the cardio-pulmonary and immune systems. An attempt has been made in this paper to elucidate the mechanisms underpinning the complex interplay between lipid delivered hydrophobic phyto-molecules, systemic lymphatics and the Immune system.

SUBMITTER: Bali S

PROVIDER: S-EPMC8728051 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:BackgroundNayopayam kwatha (NK) is a well-known polyherbal formulation widely used to cure respiratory ailments, heart problems, and postnatal difficulties. Literature suggests that so far no standardization protocol was developed for NK to validate its quality and purity.Objective(s)To develop a standardization protocol for NK based on the marker phytoconstituents present in the individual herbs of the formulation.Materials and methodsThe roots of bala [Sida cordifolia (B1) and Sida retusa (B2)], seeds of jeeraka (Cuminum cyminum), and rhizomes of nagara (Zingiber officinale) were the ingredients of NK. Since there were two source plants for bala, two sets of NK (NKB1 and NKB2) were prepared in the ratio 3:2:1 as per Vaidya Manorama and 10:1:1 as per Arogyaraksha Kalpadruma along with 1:1:1 as per the general way of Ayurvedic polyherbal decoctions. Both the individual herbs and the kwatha (decoction) prepared were analyzed in terms of pharmacognostical, organoleptic, and physcicochemical parameters as per the standard methods. Phytochemical analysis of the individual herbs resulted in the isolation of major phytoconstituents and the kwatha was quantified in terms of marker compounds with the aid of HPLC.ResultsHPLC quantification suggests that appreciable amount of marker phytoconstituents of individual herbs are present in the kwatha. Thus, the isolated compounds luteolin (C. cyminum), 6-gingerol (Z. officinale), β-sitosterol (S. retusa), and ecdysterone (S.cordifolia) can be used as markers to standardize NK.ConclusionCharacteristics of NK, as well as its individual drugs, were well-established. The present study of NK with respect to its phytochemistry revealed that the classical drug ratios of the polyherbal formulation are of utmost importance rather than the ingredients in equal proportion. The characterization parameters of individual herbs and kwatha described in this study may serve as a standard reference for quality control analysis of NK and the method developed in this study can be used as a reliable technique for standardization of NK to ensure the purity and quality of raw drugs used.

Project description:The intracellular unbound drug concentration (Cu,cell) drives pharmacological and toxicological responses for targets inside cells. We have previously shown that Cu,cell is not always equal to extracellular unbound drug concentrations (e.g. plasma concentrations). However, the underlying mechanisms that drive cellular drug binding are poorly understood. The aim of this study was to evaluate drug binding to individual cellular components, such as neutral lipids (NL) and phospholipids (PL). The fibroblastic 3T3-L1 cell line was used as a cellular model. The cells were either used as wild-type (WT cells) or were treated with a differentiation cocktail that induced an adipocyte-like phenotype with large NL droplets (NL+PL+ cells), or treated with propranolol to induce accumulation of PL (PL+ cells). The three cell types were analysed for morphology, global protein expression, lipid content, cellular volume and lysosomal appearance. The cells were exposed to 23 drugs with diverse physicochemical properties, e.g., with regard to lipophilicity, charge, molecular weight and polar surface area. The cellular binding (fu,cell) and the total accumulation ratio (Kp) were measured and used to obtain the intracellular bioavailability (Fic)—defined as the unbound fraction of the drug concentration added to the cells that is available for intracellular target interaction. The NL+PL+ cells had an adipocyte-like morphology, whereas the PL+ were not visually distinguishable from WT cells. Analysis of the global proteome combined with pathway analysis supported the morphological appearances and confirmed the adipocyte-like phenotype of NL+PL+ cells and the normal morphology of PL+ cells. Fic was significantly altered in both treated cell types as compared to WT. A strong negative correlation between fu,cell and PL content in the cell homogenates was observed, whereas the increased NL content in the NL+PL+ cells did not increase binding further. The importance of PLs for drug binding was confirmed by affinities to beads coated with purified PLs. The NL+PL+ cells lacked acidic subcellular compartments (i.e., endo-lysosomal space), which further influenced the subcellular distribution of cationic drugs. In conclusion, our results suggest that PL content, but not NL content, is a major determinant of drug binding in cells, and that PL beads may constitute a simple alternative to more cumbersome cell distribution studies.

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Ayurvedic lipid based rasayans - A perspective on the preparation and pharmacological significance of lipids on the bioavailability of phytoconstituents.

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