Ficus benghalensis as Potential Inhibitor of 5α-Reductase for Hair Growth Promotion: In Vitro, In Silico, and In Vivo Evaluation

The screening of hair follicles, dermal papilla cells, and keratinocytes through in vitro, in vivo, and histology has previously been reported to combat alopecia. Ficus benghalensis has been used conventionally to cure skin and hair disorders, although its effect on 5α-reductase II is still unknown. Currently, we aim to analyze the phytotherapeutic impact of F. benghalensis leaf extracts (FBLEs) for promoting hair growth in rabbits along with in vitro inhibition of the steroid isozyme 5α-reductase II. The inhibition of 5α-reductase II by FBLEs was assessed by RP-HPLC, using the NADPH cofactor as the reaction initiator and Minoxin (5%) as a positive control. In silico studies were performed using AutoDock Vina to visualize the interaction between 5α-reductase II and the reported phytoconstituents present in FBLEs. Hair growth in female albino rabbits was investigated by applying an oral dose of the FBLE formulation and control drug to the skin once a day. The skin tissues were examined by histology to see hair follicles. Further, FAAS, FTIR, and antioxidants were performed to check the trace elements and secondary metabolites in the FBLEs. The results of RP-HPLC and the binding energies showed that FBLEs reduced the catalytic activity of 5α-reductase II and improved cell proliferation in rabbits. The statistical analysis (p 70%) suggested that hydroalcoholic FBLE has more potential in increasing hair growth by elongating hair follicle’s anagen phase. FAAS, FTIR, and antioxidant experiments revealed sufficient concentrations of Zn, Cu, K, and Fe, together with the presence of polyphenols and scavenging activity in FBLE. Overall, we found that FBLEs are potent in stimulating hair follicle maturation by reducing the 5α-reductase II action, so they may serve as a principal choice in de novo drug designing to treat hair loss

A novel pH-responsive hydrogel system based on Prunus armeniaca gum and acrylic acid: Preparation and evaluation as a potential candidate for controlled drug delivery

pH-responsive hydrogels have become effective and attractive materials for the controlled release of drugs at pre-determined destinations. In the present study, a novel hydrogel system based on Prunus armeniaca gum (PAG) and acrylic acid (AA) was prepared by a free radical mechanism using N, N-methylene bisacrylamide (MBA) as cross-linker and potassium persulfate (KPS) as initiator. A series of hydrogels varying PAG, AA, and MBA concentration was developed to determine the impact of these components. Formulated hydrogels were characterized for pH-responsive swelling, drug release, gel content, and porosity. Structural analysis was performed by FTIR, XRD, and SEM analysis. TGA study was applied to assess thermal stability. Oral acute toxicity and in vivo drug release were performed in rabbits. Hydrogels exhibited pH-dependent swelling and drug release. Swelling, drug loading and release, and porosity increased by increasing PAG and AA concentration while decreased by increasing MBA. The gel content of formulations was increased by increasing all three components. FTIR studies confirmed the development of copolymeric networks and the loading of drug. XRD studies revealed that hydrogels were amorphous, and the crystalline drug was changed into an amorphous form during loading. TGA results indicated that hydrogels were stable up to 600 °C. Acute oral toxicity results confirm that hydrogels were nontoxic up to a dose of 2 g/kg body weight in rabbits. The pharmacokinetic evaluation revealed that hydrogels prolonged the availability of the drug and the peak plasma concentration of the drug was obtained in 6 h as compared to the oral solution of the drug. Tramadol hydrochloride (THC) was used as a model drug. Hence, pH-responsive swelling and release, nontoxic nature and improved pharmacokinetics support that PAG-based hydrogels may be considered as potential controlled-release polymeric carriers

Seeds of Giant Dodder (Cuscuta reflexa) as a Function of Extract Procedure and Solvent Nature

Seeds of a renowned medicinal plant, giant dodder (Cuscuta reflexa), were assessed to appraise the effect of solvent and extraction technique variation on antioxidants potential. Dodder seed, also called cuscuta seed, has been considered superb tonic in traditional herbal medication for eyes, liver, spleen and kidney. Results show that selected solvent and procedure plays a key role in the composition and activity of extractable material. Three extraction procedures Orbital shaker, Decoction and Ultrasonic assisted extraction and five different solvents n-hexane, ethyl acetate, 100% methanol, 80% methanol and 60% methanol were used to get optimized conditions. Total phenolic and flavonoids content were found maximum in the extracts of aqueous organic system containing 80% methanol in Ultrasonic assisted extraction method but in case of tannins ethyl acetate and Orbital shaker extraction was found more suitable partner. Antioxidant estimation assays showed a little bit variation as DPPH and ABTS exhibited maximum inhibition in 80% methanol and Ultrasonic assisted extraction but 100% methanol was found better for FRAP assay. Decoction results were mostly in between the both Orbital shaker and Ultrasonic assisted extraction. Overall results indicate that coexistence of polar solvents and Ultrasonic assisted extraction gives a better choice for extractability of potent antioxidants from seeds. HPLC analysis confirmed presence of valuable phenolic acids. Pearson’s correlation coefficient reveals a significant relationship between extracted components and antioxidant capacity P< 0.05 or 0.01

Prunus armeniaca Gum-Alginate Polymeric Microspheres to Enhance the Bioavailability of Tramadol Hydrochloride: Formulation and Evaluation

International audienceCombinations of polymers can improve the functional properties of microspheres to achieve desired therapeutic goals. Hence, the present study aimed to formulate Prunus armeniaca gum (PAG) and sodium alginate microsphere for sustained drug release. Blended and coated microspheres were prepared using the ionotropic gelation technique. The effect of polymer concentration variation was studied on the structural and functional properties of formulated microspheres. FTIR, XRD, and thermal analysis were performed to characterize the microspheres. All the formulations were well-formed spherical beads having an average diameter from 579.23 +/- 07.09 to 657.67 +/- 08.74 mu m. Microspheres entrapped drugs within the range 65.86 +/- 0.26-83.74 +/- 0.79%. The pH-dependent swelling index of coated formulations was higher than blended. FTIR spectra confirmed the presence of characteristic peaks of entrapped Tramadol hydrochloride showing no drug-polymer interaction. In vitro drug release profile showed sustained release following the Korsmeyer-Peppas kinetic model with an R-2 value of 0.9803-0.9966. An acute toxicology study employing the oral route in Swiss albino mice showed no signs of toxicity. It can be inferred from these results that blending PAG with sodium alginate can enhance the stability of alginate microspheres and improve its drug release profile by prolonging the release time

Chitosan-Linseed mucilage polyelectrolyte complex nanoparticles of Methotrexate: In vitro cytotoxic efficacy and toxicological studies

The goal of this research was to develop, fabricate and analyze polymeric nanoparticles for the administration of methotrexate (MTX). Linseed mucilage and chitosan nanoparticles (NPs) were prepared using a slightly modified polyelectrolyte complex (PEC) method. The size, shape, and encapsulation effectiveness of the resultant nanoparticles were measured. MTX release profiles at gastrointestinal pH (1.2 and 7.4) and tumor pH (5.5) were examined to determine the targeted potential of NPs as pH-responsive nanocarriers. Zeta analysis showed that nanoparticles prepared by PEC have a size range of 192.1 nm to 246 nm, and PDI was 0.3 of the optimized formulation, which showed homogenous nature of prepared nanoparticles formulation. The findings demonstrated that NPs have a low polydispersity index and a positive zeta potential (PDI). The in-vitro release of the drug indicated a pH-dependent, sustained drug release up to 24 h. Blank LSMCSNPs had almost no in-vivo cytotoxicity for 14 days, while optimum MTX loaded NPs had strong antitumor effects on HepG2 and MCF-7 cells as measured by the MTT assay. Cell apoptosis induction was also checked and MCF-7 cells treated with MTX-LSMCSNPs had a significantly greater rate of apoptosis (21.2 %) than those treated with MTX alone (14.14 %). The findings show that LSMCSNPs could be a potential delivery mechanism for methotrexate to cancer cells in a secure, steady, and ideally controlled manner to improve therapeutic outcomes

Synthesis of pH-Sensitive Cross-Linked Basil Seed Gum/Acrylic Acid Hydrogels by Free Radical Copolymerization Technique for Sustained Delivery of Captopril

The pH-sensitive polymeric matrix of basil seed gum (BSG), with two different monomers, such as acrylic acid (AA) and N, N-Methylene-bis-acrylamide (MBA), was selected to use in hydrogels preparation through a free radical copolymerization technique using potassium per sulfate (KPS) as a cross linker. BSG, AA and MBA were used in multiple ratios to investigate the polymer, monomer and initiator effects on swelling properties and release pattern of captopril. Characterization of formulated hydrogels was done by FTIR, DSC/TGA, XRD and SEM techniques to confirm the stability. The hydrogels were subjected to a variety of tests, including dynamic swelling investigations, drug loading, in vitro drug release, sol–gel analyses and rheological studies. FTIR analysis confirmed that after the polymeric reaction of BSG with the AA monomer, AA chains grafted onto the backbone of BSG. The SEM micrographs illustrated an irregular, rough, and porous form of surface. Gel content was increased by increasing the contents of polymeric gum (BSG) with monomers (AA and MBA). Acidic and basic pH effects highlighted the difference between the swelling properties with BSG and AA on increasing concentration. Kinetic modelling suggested that Korsmeyer Peppas model release pattern was followed by the drug with the non-Fickian diffusion mechanism

pH Responsive Abelmoschus esculentus Mucilage and Administration of Methotrexate: In-Vitro Antitumor and In-Vivo Toxicity Evaluation

International audienceThe rapid progression in biomaterial nanotechnology apprehends the potential of non-toxic and potent polysaccharide delivery modules to overcome oral chemotherapeutic challenges. The present study is aimed to design, fabricate and characterize polysaccharide nanoparticles for methotrexate (MTX) delivery. The nanoparticles (NPs) were prepared by Abelmoschus esculentus mucilage (AEM) and chitosan (CS) by the modified coacervation method, followed by ultra-sonification. The NPs showed much better pharmaceutical properties with a spherical shape and smooth surface of 213.4-254.2 nm with PDI ranging between 0.279-0.485 size with entrapment efficiency varying from 42.08 ± 1.2 to 72.23 ± 2.0. The results revealed NPs to possess positive zeta potential and a low polydispersity index (PDI). The in-vitro drug release showed a sustained release of the drug up to 32 h with pH-dependence. Blank AEM -CS NPs showed no in-vivo toxicity for a time duration of 14 days, accompanied by high cytotoxic effects of optimized MTX loaded NPs against MCF-7 and MD-MBA231 cells by MTT assay. In conclusion, the findings advocated the therapeutic potential of AEM/CS NPs as an efficacious tool, offering a new perspective for pH-responsive routing of anticancer drugs with tumor cells as a target

Formulation and evaluation of quince seeds mucilage - sodium alginate microspheres for sustained delivery of cefixime and its toxicological studies

International audienceQuince seed mucilage was used in a combination of sodium alginate to develop sustained-release microspheres of cefixime. Physical characterizations such as FTIR, TGA, DSC, and SEM were performed on the prepared microspheres. The swelling of microspheres was maximum at pH 7.4 and reduced at acidic pH. The average particle size ranged from 679 mu m +/-and nbsp;0.21 to 810 mu m +/-and nbsp;0.31, while the drug encapsulation efficiency range was found as 73.76 +/- 0.24-85.6 3 +/- 0.46. In vitro release profile of QSM-alginate-cefixime microspheres followed Korsmeyer-Peppas model (R-2 = 0.9732-0.9946); and release was non-Fickian as we found value of n > 1. This study reveals the benefits of QSM-alginate microspheres for the sustained release of cefixime without any toxicity and it also improved antibacterial properties. (C)and nbsp;2022 The Authors. Published by Elsevier B.V. on behalf of King Saud University

Polymeric complex nanocarriers of Mangifera indica gum & chitosan for methotrexate delivery: Formulation, characterization, and in vitro toxicological assessment

Methotrexate (MTX), a widely used chemotherapeutic drug, exhibits significant potential in the treatment of various solid tumors and hematologic malignancies. However, its therapeutic efficacy is often hampered by suboptimal pharmacokinetic profiles, causing drug resistance and a shortened plasma half-life. In recent years, in light of these challenges, a demand has arisen for novel strategies to augment the therapeutic potential of methotrexate. The present study presents an innovative approach in the development and evaluation of non-toxic nanocarriers designed for methotrexate delivery, using a biopolymer matrix comprised of Mangifera Indica gum (MIG) and chitosan (CS), employing the coacervation technique. The optimization process, guided by central composite design, was utilized to attain an optimal formulation containing 0.02% w/v% MIG and 0.01% w/v% CS. The characterization of optimized formulation revealed smooth, spherical nanoparticles (229.7 nm diameter, PDI 0.296) with 69.5 ± 2.0% entrapment efficiency. Additionally, a pH-dependent sustained release of the MTX for up to 24 h was found using in-vitro drug release analysis. Furthermore, the optimized formulation displayed significant cytotoxic effects in an MTT assay, highlighting its potential as an effective carrier for the delivery MTX to cancer cells. These findings offer valuable insights into pH-responsive drug delivery to tumor cells and underscore the promising therapeutic efficacy of MIG/CS nanoparticles, positioning them as a compelling option for novel pharmaceutical formulations

Maximizing the extraction yield of plant gum exudate using response surface methodology and artificial neural networking and pharmacological characterization

Abstract Prunus armeniaca gum is used as food additive and ethno medicinal purpose. Two empirical models response surface methodology and artificial neural network were used to search for optimized extraction parameters for gum extraction. A four-factor design was implemented for optimization of extraction process for maximum yield which was obtained under the optimized extraction parameter (temperature, pH, extraction time, and gum/water ratio). Micro and macro-elemental composition of gum was determined by using laser induced breakdown spectroscopy. Gum was evaluated for toxicological effect and pharmacological properties. The maximum predicted yield obtained by response surface methodology and artificial neural network was 30.44 and 30.70% which was very close to maximum experimental yield 30.23%. Laser induced breakdown spectroscopic spectra confirmed the presence Calcium, Potassium, Magnesium, Sodium, Lithium, Carbon, Hydrogen, Nitrogen and Oxygen. Acute oral toxicity study showed that gum is non-toxic up to 2000 mg/Kg body weight in rabbits, accompanied by high cytotoxic effects of gum against HepG2 and MCF-7cells by MTT assay. Overall, Aqueous solution of gum showed various pharmacological activities with significant value of antioxidant, antibacterial, anti-nociceptive, anti-cancer, anti-inflammatory and thrombolytic activities. Thus, optimization of parameters using mathematical models cans offer better prediction and estimations with enhanced pharmacological properties of extracted components