Revisiting the significance of nano-vitamin D for food fortification and therapeutic application.

OBJECTIVE: Vitamin D (a prohormone) is an important micronutrient required by the body for skeletal homeostasis and a range of non-skeletal actions. Calcitriol, the active form of vitamin D, regulates a variety of cellular and metabolic processes through both genomic and nongenomic pathways. Often prescribed for treating rickets and osteoporosis, vitamin D deficiency can exacerbate various other medical conditions. SIGNIFICANCE, METHODS, AND RESULTS: Despite its multifunctional uses, the sensitivity of vitamin D makes formulating an efficient drug delivery system a challenging task, which is further complicated by its poor aqueous solubility. Enhancing the oral absorption of vitamin D is vital in utilizing its full efficacy. Recent developments in encapsulation and nanotechnology have shown promising results in overcoming these constraints. CONCLUSION: This review thus offers an insight to adequately comprehend the mechanistic pharmacology of vitamin D, its pathophysiological role, and justification of its medical indications, along with the benefits of utilizing nanotechnology for vitamin D delivery.

Combinatorial drug-loaded quality by design adapted transliposome gel formulation for dermal delivery: In vitro and dermatokinetic study.

BACKGROUND: Ursolic acid is a powerful drug that possesses many therapeutic properties, such as hepatoprotection, immunomodulation, anti-inflammatory, antidiabetic, antibacterial, antiviral, antiulcer, and anticancer activity. Centella asiatica (L.) Urban (Umbelliferae) contains a triterpene called asiatic acid, which has been used effectively in traditional Chinese and Indian medicine system for centuries. Anticancer, anti-inflammatory, and neuroprotective properties are only some of the many pharmacological actions previously attributed to asiatic acid . AIM: The present work developed an optimized combinatorial drug-loaded nano-formulation by Quality by design approach. MATERIALS AND METHODS: The optimize transliposome for accentuated dermal delivery of dual drug. The optimization of drug-loaded transliposome was done using the "Box-Behnken design." The optimized formulation was characterized for vesicles size, entrapment efficiency (%), and in vitro drug release. Additionally, transmission electron microscopy (TEM), confocal laser scanning microscopy (CLSM), and dermatokinetic study were performed for further evaluation of drug-loaded optimized transliposome formulation. RESULTS: The optimized combinatorial drug-loaded transliposome formulation showed a particle size of 86.36 ± 2.54 nm, polydispersity index (PDI) 0.230 ± 0.008, and an entrapment efficiency of 87.43 ± 2.66% which depicted good entrapment efficiency. In vitro drug release of ursolic acid and asiatic acid transliposomes was found to be 85.12 ± 2.54% and 80.23 ± 3.23%, respectively, as compared to optimized ursolic acid and asiatic acid transliposome gel drug release that was 67.18 ± 2.85% and 60.28 ± 4.12%, respectively. The skin permeation study of ursolic and asiatic acid conventional formulation was only 32.48 ± 2.42%, compared with optimized combinatorial drug-loaded transliposome gel (79.83 ± 4.52%) at 12 h. After applying combinatorial drug-loaded transliposome gel, rhodamine was able to more easily cross rat skin, as observed by confocal laser scanning microscopy, in comparison with when the rhodamine control solution was used. DISCUSSION: The UA_AA-TL gel formulation absorbed more ursolic acid and asiatic acid than the UA_AA-CF gel formulation, as per dermatokinetic study. Even after being incorporated into transliposome vesicles, the antioxidant effects of ursolic and asiatic acid were still detectable. In most cases, transliposomes vesicular systems generate depots in the skin's deeper layers and gradually release the medicine over time, allowing for fewer applications. CONCLUSION: In overall our studies, it may be concluded that developed dual drug-loaded transliposomal formulation has great potential for effective topical drug delivery for skin cancer.

Fabrication of Sustained Release Curcumin-Loaded Solid Lipid Nanoparticles (Cur-SLNs) as a Potential Drug Delivery System for the Treatment of Lung Cancer: Optimization of Formulation and In Vitro Biological Evaluation.

The goal of current research was to develop a new form of effective drug, curcumin-loaded solid lipid nanoparticles (Cur-SLNs) and test its efficacy in the treatment of lung cancer. Different batches of SLNs were prepared by the emulsification-ultrasonication method. For the optimization of formulation, each batch was evaluated for particle size, polydispersity index (PI), zeta potential (ZP), entrapment efficiency (EE) and drug loading (DL). The formulation components and process parameters largely affected the quality of SLNs. The SLNs obtained with particle size, 114.9 ± 1.36 nm; PI, 0.112 ± 0.005; ZP, -32.3 ± 0.30 mV; EE, 69.74 ± 2.03%, and DL, 0.81 ± 0.04% was designated as an optimized formulation. The formulation was freeze-dried to remove excess water to improve the physical stability. Freeze-dried Cur-SLNs showed 99.32% of drug release and demonstrated a burst effect trailed by sustained release up to 120 h periods. The erythrocyte toxicity study of Cur-SLNs and its components demonstrated moderate hemolytic potential towards red blood cells (RBCs). The cytotoxic potential of the formulation and plain curcumin was estimated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against A549 cell line. After 48 h of incubation, Cur-SLNs demonstrated more cytotoxicity (IC50 = 26.12 ± 1.24 µM) than plain curcumin (IC50 = 35.12 ± 2.33 µM). Moreover, the cellular uptake of curcumin was found to be significantly higher from Cur-SLNs (682.08 ± 6.33 ng/µg) compared to plain curcumin (162.4 ± 4.2 ng/µg). Additionally, the optimized formulation was found to be stable over the period of 90 days of storage. Hence, curcumin-loaded SLNs can be prepared using the proposed cost effective method, and can be utilized as an effective drug delivery system for the treatment of lung cancer, provided in vivo studies warrant a similar outcome.

Nano Matrix Soft Confectionary for Oral Supplementation of Vitamin D: Stability and Sensory Analysis.

Vitamin D deficiency distresses nearly 50% of the population globally and multiple studies have highlighted the association of Vitamin D with a number of clinical manifestations, including musculoskeletal, cardiovascular, cerebrovascular, and neurological disorders. In the current study, vitamin D oil-in-water (O/W) nanoemulsions were developed and incorporated in edible gummies to enhance bioavailability, stability, and patient compliance. The spontaneous emulsification method was employed to produce a nano-emulsion using corn oil with tween 20 and lecithin as emulsifiers. Optimization was carried out using pseudo-ternary phase diagrams and the average particle size and polydispersity index (PDI) of the optimized nanoemulsion were found to be 118.6 ± 4.3 nm and 0.11 ± 0.30, respectively. HPLC stability analysis demonstrated that the nano-emulsion prevented the degradation and it retained more than 97% of active vitamin D over 15 days compared to 94.5% in oil solution. Similar results were obtained over further storage analysis. Vitamin D gummies based on emulsion-based gelled matrices were then developed using gelatin as hydrocolloid and varying quantities of corn oil. Texture analysis revealed that gummies formulated with 10% corn oil had the optimum hardness of 3095.6 ± 201.7 g on the first day which remained consistent on day 45 with similar values of 3594.4 ± 210.6 g. Sensory evaluation by 19 judges using the nine-point hedonic scale highlighted that the taste and overall acceptance of formulated gummies did not change significantly (p > 0.05) over 45 days storage. This study suggested that nanoemulsions consistently prevent the environmental degradation of vitamin D, already known to offer protection in GI by providing sustained intestinal release and enhancing overall bioavailability. Soft chewable matrices were easy to chew and swallow, and they provided greater patient compliance.

Identification of the Phytoconstituents in Methanolic Extract of Adhatoda Vasica L. Leaves by GC-MS Analysis and Its Antioxidant Activity.

BACKGROUND: Adhatoda vasica L. is a medicinal plant, known as Malabar nut in English, belonging to the family Acanthaceae. It has been used traditionally to treat respiratory disorders like severe coughs, colds, chronic bronchitis, asthma, tuberculosis, and other illnesses. The multifunctional range of bioactives found in it has piqued the interest of pharmaceutical companies, who are looking for more evidence-based ways to develop new formulations. OBJECTIVE: To analyse the A. vasica leaves by GC-MS technique and evaluation of its antioxidant activity. METHOD: Methanolic extract of A. vasica L. (MEAV) leaves was analyzed by GC-MS for identification and characterization of its bioactives and traditional therapeutic claims. A widely anticipated 2,2-diphenyl-1-picrylhydrazyl (DPPH) method was used to determine the antioxidant activity of MEAV. RESULTS: The major compounds revealed in MEAV leaves are: 1,3,5-triazine-2,4,6-triamine (3.06%); 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (5.35%); 5-hydroxymethylfurfural (16.82%); 2-butylphenol (6.85%); 3,4-dihydroxy-5-methyl-dihydro-furan-2-on (2.5%); 2(OR 3)-(1,1-dimethylethyl)-4-methoxyphenol (3.52%); megastigmatrienone 3 (1.02%); tetradecanoic acid (1.52%); vomifoliol (0.58%); oxalic acid, cyclobutylhexyl ester (6.03%); hexadecanoic acid (6.06%); 4-ethyl-2-oxo-2,5,6,7-tetrahydro-1H-cyclopenta[B]pyridine-3-carbonitrile (10.08%); phytol (2.01%); and vitamin E (3.18%). A significant reduction in free radicals against DPPH was observed, which revealed the antioxidant potential of MEAV. CONCLUSION: MEAV consists of both polar and nonpolar components. GC-MS analysis was used to identify these compounds. The current work validates that the antioxidant activity of MEAV is attributed to the presence of compounds such as vitamin E and terpenes. HIGHLIGHTS: This work validates the antioxidant activity of methanolic extract of A. vasica attributed to the presence of compounds like vitamin E and terpenes.

Phytochemical-Based Nano-Pharmacotherapeutics for Management of Burn Wound Healing.

Medicinal plants have been used since ancient times for their various therapeutic activities and are safer compared to modern medicines, especially when properly identifying and preparing them and choosing an adequate dose administration. The phytochemical compounds present in plants are progressively yielding evidence in modern drug delivery systems by treating various diseases like cancers, coronary heart disease, diabetes, high blood pressure, inflammation, microbial, viral and parasitic infections, psychotic diseases, spasmodic conditions, ulcers, etc. The phytochemical requires a rational approach to deliver the compounds to enhance the efficacy and to improve patients' compatibility. Nanotechnology is emerging as one of the most promising strategies in disease control. Nano-formulations could target certain parts of the body and control drug release. Different studies report that phytochemical-loaded nano-formulations have been tested successfully both in vitro and in vivo for healing of skin wounds. The use of nano systems as drug carriers may reduce the toxicity and enhance the bioavailability of the incorporated drug. In this review, we focus on various nano-phytomedicines that have been used in treating skin burn wounds, and how both nanotechnology and phytochemicals are effective for treating skin burns.

Antimicrobial activity of different plants extracts against Staphylococcus aureus and Escherichia coli.

BACKGROUND: Microbial pathogens, mainly bacteria, are a major cause of food spoilage resulting in several foodborne diseases. Food spoilage can be prevented by the application of chemical preservatives in the food industry but such process has harmful effects on human health and causes the introduction of chemicals in several food chains, leading to toxicity and long-term complications. Due to such adverse effects, the need to find natural preservatives that are safer to use, effective and less complicated is increasing. OBJECTIVES: This study is based on plant extracts that play a major role in microbicidal action (the use of natural preservatives is preferred over chemical ones). Antimicrobial action of different plant extracts was assessed using Staphylococcus aureus and Escherichia coli as experimental bacterial strains. MATERIAL AND METHODS: Ethanolic extracts of different plants like Punica granatum, Acacia catechu and Phyllanthus emblica were highly effective against the both analyzed bacterial strains at a dosage of 10 mg/mL, while the extracts of Ocimum bacilicum and Quercus infectoria were effective only against S. aureus and E. coli, respectively. RESULTS: Punica granatum and Phyllanthus emblica extracts were found to be the most effective and exhibited bacteriostatic and bactericidal activities against the highly infectious strains of pathogenic bacteria causing food spoilage, with minimum inhibitory concentration (MIC) of 2.5 mg/mL and minimum bactericidal concentration (MBC) of 5 mg/mL. CONCLUSIONS: The plant extracts used in the study were highly effective in reducing bacterial contamination and can be used as an alternative to chemical preservatives to avoid and control foodborne diseases and for preservation of food with no health-related hazards caused by chemicals.

GC-MS Analysis and Antioxidant Activity of Wrightia tinctoria R.Br. Leaf Extract.

BACKGROUND: Wrightia tinctoria R.Br. (Apocyanaceae) is known as a biologically effective plant for the treatment of jaundice in the Indian traditional system of medicine. It is a wild medicinal tree possessing anti-inflammatory, antidiabetic, antinociceptive, hepatoprotective, antibacterial, antifungal, antiviral, antipsoriatic, anticancerous, anthelmintic, aphrodisiac, analgesic, and antipyretic activities. Its constituents are of utmost interest to pharmaceutical industries owing to their many actions and biological activities. METHOD: Methanolic extract of W. tinctoria (MEWT) was investigated by gas chromatography-mass spectroscopy and provided affirmative results assisting in the identification and characterization of therapeutic claims regarding this species in the traditional system. The antioxidant activity of MEWT was determined by the most suitable DPPH method. RESULTS: The basic compounds found in MEWT were ß-caryophyllene (0.22%), mome inositol (12.02%), neophytadiene (1.61%), eicosanoic acid methyl ester (0.32%), 8,11,14-eicosatrienoic acid methyl ester (0.60%), phytol (0.94%), phytol palmitate (1.37%), squalene (1.57%), flavone 4-OH, 5-OH, 7-di-O-glucoside (29.34%), γ-tocopherol (0.49%), stigmast-5-en-3-ol (3.14%), methyl commate B (1.76%), methyl commate A (5.20%), and 24-norursa-3,12-diene (20.36%). The obtained results in the analysis of antioxidant activity of MEWT exhibited considerable free radical scavenging capacity against DPPH-generated free radicals. CONCLUSIONS: This study expands the knowledge of MEWT chemical composition and provides evidence to substantiate ethno-medicinal use of the plant by exploring antioxidant activity. The substantial antioxidant activity of MEWT could be due to presence of terpenes, flavonoids, vitamin E, and other reported compounds. HIGHLIGHTS: This study includes identification of phytochemicals and antioxidant potential of methanolic extract of Wrightia tinctoria, assisting in therapeutic claims regarding this species in the traditional system.

Omega-3 fatty acids as adjunctive therapeutics: prospective of nanoparticles in its formulation development.

Omega-3 polyunsaturated fatty acids (ω-3-PUFAs) are dietary components that have been extensively recognized for their therapeutic value and have shown diverse therapeutic effects including anti-inflammatory, antiarrhythmic, antithrombotic, immunomodulatory and antineoplastic activities. Most of the ω-3-PUFAs are obtained through diet or supplements because the body does not synthesize them. The high instability of ω-3-PUFAs to oxidative deterioration, lower bioavailability at the target tissues and reduced bioactivity of ω-3-PUFAs is an impediment for achieving their therapeutic potential. The present review provides an overview of potential therapeutic activities of ω-3-PUFAs and different novel technical approaches based on nanotechnology, which have been emphasized to overcome instability problems as well as enhance the bioactivity of ω-3-PUFAs. Future prospects related to this area of research are also provided.

Transformation of curcumin from food additive to multifunctional medicine: nanotechnology bridging the gap.

Curcumin (CUR) is a yellow-coloured polyphenolic compound obtained from the rhizomes of Curcuma longa. In-depth pharmacological screening of curcumin has given the evidence that CUR persuades shielding and curative effects against various cancers, cardiovascular, wound healing effect and neuro disorders etc owning to anti-oxidant, antiproliferative, anti-inflammatory, anti-angiogenic and antimicrobial activities. However, miserable bioavailability due to poor aqueous solubility limits the application of CUR in various ailments. Different methodologies including the nanoparticle technology have been reported for the bioavailability enhancement of CUR. Nanoparticles exhibit not only the improvement in the solubility of CUR and alike lipophilic molecules (resulted in improved bioavailability) but also giving the opportunity for the disease specific cellular and organ targeting. Improved bioavailability and disease based site specific delivery of CUR is more likely to bring it as a safe multifunctional medicine.