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.

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.

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.

GC-MS analysis of the methanolic extracts of Smilax china and Salix alba and their antioxidant activity.

Smilax china L. (family Smilacaceae) and Salix alba L. (family Salicaceae) are plants that have been traditionally used to treat various ailments in Indian and Chinese medicine. A quantitative estimation of the methanolic extracts of these plants was performed by GC-MS analysis to obtain insight into its phytoconstituents responsible for therapeutic action. The antioxidant potential of the methanol extracts of Smilax china (MESC) and Salix alba (MESA) were assessed with DPPH by using a UV spectrophotometer at a wavelength of 517 nm. The prevailing compounds found in MESC were lactam sugars including 2,5-dimethyl-2,4-dihydroxy-3(2H)-furanon (1.40%), 1,5-anhydro-6-deoxyhexo-2,3-diulose (4.33%), and alpha-methyl-1-sorboside (1.80%); the two alkaloids found were 1,4-methane-4,4a,5,6,7,8,9,9a-octahydro-10,10-dimethyl cyclohepta[d] pyridazine (0.87%) and 1,3,7-trimethyl-2,6-dioxopurine(0.54%); terpenes included deltacadinene (0.39%), terpineol, (+)-cedrol (22.13%), 3-thujanol (0.77%), and 9,10-dehydro-cycloisolongifolene (0.34%); fatty acids included cis-vaccenic acid (4.98%) and telfairic acid (1.10%); esters included 1,2,3-propanetriol diacetate (7.56%), 7-hexadecenoic acid, methyl ester (1.77%), eicosanoic acid, and methyl ester (0.95%); and glycerol included 1,2,3-propanetriol (28.75%). The interesting compounds found in MESA were reducing sugars like D-allose (4.40%) and pyrogallol (10.48%), alkaloids like caffeine (63.49%), and esters like methyl octadecanoate (0.53%). Both fractions revealed considerable antioxidant activity. The reported existing phenolic compounds and terpenes are responsible for the antioxidant activity of the plant extracts.

TLC-Bioautographic Evaluation for High-Throughput Screening and Identification of Free Radical Scavenging and Antidiabetic Compounds from Traditional Unani Medicinal Plant: Citrullus colocynthis Schrad.

BACKGROUND: Interest in the antioxidant and antidiabetic activity of natural products are growing vastly in the modern world. Thin layer chromatography-bioautography-mass spectroscopy (TLC-bioautography-MS) plays an important role in chemico-biological screening of natural sources. TLC combined with 2, 2-Diphenyl-1-picrylhydrazyl (DPPH) free radical, α-amylase and α-glucosidase bioassay were used to evaluate antioxidant and antidiabetic activities, respectively, in different extracts of Citrullus colocynthis (Hanzal), a well-known traditional Indian Unani medicinal plant. OBJECTIVE: To develop a TLC-bioautographic-MS method for DPPH, α-amylase, and glucosidase inhibitors in different extract of C. colocynthis fruits. METHOD: Fruits of C. colocynthis were successively extracted with toluene, dichloromethane, ethyl acetate, methanol, and water. TLC solvents were developed, and bioautographic-MS analysis was carried out to identify the antioxidant and antidiabetic compounds. RESULTS: HPTLC fingerprinting analysis showed maximum numbers of band separated in dichloromethane and ethyl acetate extracts of C. colocynthis, fourteen and thirteen at 254 and 366 nm, respectively. Whereas six and five separated bands were observed in toluene extract at 254 and 366 nm, respectively showed minimum numbers of metabolites. Based on TLC-bioautography-MS, maximum number of antioxidant compounds were identified in dichloromethane extract. Except aqueous extract of C. colocynthis, all the extracts have shown antidiabetic activity. On the other hand, there were no antioxidant compounds in methanolic extract of C. colocynthis. CONCLUSIONS: The results of this study reveal that TLC-bioautography-MS-guided strategy used to identify antioxidant and antidiabetic compounds of C. colocynthis is very useful technique for high-throughput screening of bioactive compounds. HIGHLIGHTS: TLC-MS bioautography is a simple and fast to enables bioactive compounds present in extracts.