Lipid Nanoparticles: An Effective Tool to Improve the Bioavailability of Nutraceuticals.

Nano-range bioactive colloidal carrier systems are envisaged to overcome the challenges associated with treatments of numerous diseases. Lipid nanoparticles (LNPs), one of the extensively investigated drug delivery systems, not only improve pharmacokinetic parameters, transportation, and chemical stability of encapsulated compounds but also provide efficient targeting and reduce the risk of toxicity. Over the last decades, nature-derived polyphenols, vitamins, antioxidants, dietary supplements, and herbs have received more attention due to their remarkable biological and pharmacological health and medical benefits. However, their poor aqueous solubility, compromised stability, insufficient absorption, and accelerated elimination impede research in the nutraceutical sector. Owing to the possibilities offered by various LNPs, their ability to accommodate both hydrophilic and hydrophobic molecules and the availability of various preparation methods suitable for sensitive molecules, loading natural fragile molecules into LNPs offers a promising solution. The primary objective of this work is to explore the synergy between nature and nanotechnology, encompassing a wide range of research aimed at encapsulating natural therapeutic molecules within LNPs.

Olive oil and clove oil-based nanoemulsion for topical delivery of terbinafine hydrochloride: in vitro and ex vivo evaluation.

In this article, formulation studies for terbinafine hydrochloride nanoemulsions, prepared by high-energy ultrasonication technique, are described. Pseudo-ternary phase diagram was constructed in order to find out the optimal ratios of oil and surfactant/co-solvent mixture for nanoemulsion production. Clove and olive oils were selected as oil phase. Based on the droplet size evaluation, maximum nanoemulsion region were determined for formulation development. Further characterization included polydispersity index (PDI), zeta potential, Fourier transform infrared (FT-IR) spectroscopy, morphology, pH, viscosity, refractive index, ex vivo skin permeation, skin irritation, and histopathological examination. Droplet sizes of optimized formulations were in colloidal range. PDI values below 0.35 indicated considerably homogeneous nanoemulsions. Zeta potential values were from 13.2 to 18.1 mV indicating good stability, which was also confirmed by dispersion stability studies. Ex vivo permeation studies revealed almost total skin permeation of terbinafine hydrochloride from the nanoemulsions (96-98%) in 6 hours whereas commercial product reached only 57% permeation at the same time. Maximum drug amounts were seen in epidermis and dermis layers. Skin irritation and histopathological examination demonstrated dermatologically safe formulations. In conclusion, olive oil and clove oil-based nanoemulsion systems have potential to serve as promising carriers for topical terbinafine hydrochloride delivery.

Formulation and Evaluation of a Clove Oil-Encapsulated Nanofiber Formulation for Effective Wound-Healing.

Wound-healing is complicated process that is affected by many factors, especially bacterial infiltration at the site and not only the need for the regeneration of damaged tissues but also the requirement for antibacterial, anti-inflammatory, and analgesic activity at the injured site. The objective of the present study was to develop and evaluate the natural essential oil-containing nanofiber (NF) mat with enhanced antibacterial activity, regenerative, non-cytotoxic, and wound-healing potential. Clove essential oil (CEO) encapsulated in chitosan and poly-ethylene oxide (PEO) polymers to form NFs and their morphology was analyzed using scanning electron microscopy (SEM) that confirmed the finest NFs prepared with a diameter of 154 ± 35 nm. The successful incorporation of CEO was characterized by Fourier transform infra-red spectroscopy (FTIR) and X-ray diffractometry (XRD). The 87.6 ± 13.1% encapsulation efficiency and 8.9 ± 0.98% loading of CEO was observed. A total of 79% release of CEO was observed in acidic pH 5.5 with 117% high degree of swelling. The prepared NF mat showed good antibacterial activity against Staphylococcus aureus and Escherichia coli and non-cytotoxic behavior against human fibroblast cell lines and showed good wound-healing potential.

Enhancement of Oral Bioavailability of Ibandronate Through Gastroretentive Raft Forming Drug Delivery System: In Vitro and In Vivo Evaluation.

BACKGROUND: Bisphosphonates have very low bioavailability and cause irritation of the esophagus and stomach. This study was planned to improve the oral bioavailability of ibandronate through the formation of a raft in the stomach. Bisphosphonate-induced irritation of the esophagus and stomach is prevented by the formation of a raft. MATERIALS AND METHODS: The nanostructured raft was developed through the use of nanosized citrus pectin (NCP). The particle size of NCP was measured by zeta sizer and SEM. The percentage of NCP and the neutralization profile of raft was studied. The ibandronate, polymers, and the developed formulation were characterized by FTIR, XRD, TGA, and DSC. The release of ibandronate was studied in 0.1 N HCl, 0.5 N HCl, 1 N HCl, and simulated gastric fluid (SGF) and a cell viability study was performed using Caco-2 cells. The PPR5 formulation and Bonish 150 mg tablets were selected as test and reference formulations, respectively, for pharmacokinetic study. Twelve healthy albino rats were taken and divided into two groups using a Latin square crossover design, and the blood samples were collected for 24 hours. RESULTS: The SEM image showed that the particle size of NCP was 159 nm. The raft of PPR5 showed 94% NCP and 45 minutes duration of neutralization. The FTIR and XRD showed chemical stability and a uniform distribution of ibandronate in the raft. The TGA and DSC indicated the thermal stability of formulation. The release of 99.87% ibandronate at 20 minutes was observed in the SGF. The values of C max for the reference and test formulations were 493±0.237 ng/mL and 653±0.097 ng/mL, respectively. The AUC(0-t) of the reference and test formulations was 3708.25±3.418 ng/mL.h and 6899.25±3.467 ng/mL.h, respectively. CONCLUSION: The NCP has been successfully prepared from citrus pectin and has shown effective porous raft formation. The bioavailability of the ibandronate from newly developed PPR5 was higher than the already marketed formulation.

Progress and prospects in the management of bacterial infections and developments in Phytotherapeutic modalities.

The advent of antibiotics revolutionized medical care resulting in significantly reduced mortality and morbidity caused by infectious diseases. However, excessive use of antibiotics has led to the development of antibiotic resistance and indeed, the incidence of multidrug-resistant pathogens is considered as a major disadvantage in medication strategy, which has led the scholar's attention towards innovative antibiotic sources in recent years. Medicinal plants contain a variety of secondary metabolites with a wide range of therapeutic potential against the resistant microbes. Therefore, the aim of this review is to explore the antibacterial potential of traditional herbal medicine against bacterial infections. More than 200 published research articles reporting the therapeutic potential of medicinal plants against drug-resistant microbial infections were searched using different databases such as Google Scholar, Science Direct, PubMed and the Directory of Open Access Journals (DOAJ), etc., with various keywords like medicinal plants having antibacterial activities, antimicrobial potentials, phytotherapy of bacterial infection, etc. Articles were selected related to the efficacious herbs easily available to local populations addressing common pathogens. Various plants such as Artocarpus communis, Rheum emodi, Gentiana lutea L., Cassia fistula L., Rosemarinus officinalis, Argemone maxicana L, Hydrastis canadensis, Citrus aurantifolia, Cymbopogon citrates, Carica papaya, Euphorbia hirta, etc, were found to have significant antibacterial activities. Although herbal preparations have promising potential in the treatment of multidrug-resistant bacterial infection, still more research is required to isolate phytoconstituents, their mechanism of action as well as to find their impacts on the human body.

Development, characterization and evaluation of ginger extract loaded microemulsion: In vitro and Ex vivo release studies.

Zingeber officinale (ginger) has been used for a long time in conventional medicine for the management of many diseases most important of which is inflammatory diseases. The aim of this study was formulation of topical microemulsion system to enhance the solubility, stability and release profile of ginger extract, as it is unstable in the presence of light, air, heat and long term storage. The solubility of ginger extract in different oils, surfactants, and cosurfactants was determined in order to find the optimal components for microemulsion. Isopropyl myristate (IPM) was selected as oil phase, tween 80 and PEG 400 were selected as surfactant and co-surfactant respectively based on highest solubility values. Pseudo-ternary phase diagram was constructed in order to find out the microemulsion region. The prepared microemulsions were evaluated for pH, viscosity, conductivity, refractive index, globular size, zeta potential, polydispersity index, ginger extract content, in-vitro and ex-vivo release profiles. The formulation GE1 showed best physicochemical properties with smallest globular size (19.75nm), highest release rate and flux value. It also showed significant (p<0.05) anti-inflammatory effect as compared to reference piroxicam drug solution. It is concluded that ginger extract can be used to develop stable microemulsion system with better skin permeation and promising antiinflammatory activity.

Development, characterization and evaluation of in-vitro anti-inflammatory activity of ginger extract based micro emulsion.

Zingeber officinale is a commonly used plant which has been shown to possess anti-inflammatory activity. The active compounds present in ginger are gingerols, shagaols and paradol. The aim of this study was formulation of topical microemulsion system to enhance the solubility and stability of ginger extract, as it is unstable in the presence of light, air, heat and long term storage, and to evaluate its anti-inflammatory activity. The solubility of ginger extract in different oils, surfactants, and co-surfactants was determined in order to find the optimal components for microemulsion. IPM was selected as oil phase, tween 80 and PEG 400 were selected as surfactant and co-surfactant respectively based on highest solubility values. Pseudo-ternary phase diagram was constructed in order to find out the microemulsion region. The prepared microemulsions were evaluated for pH, viscosity, conductivity, refractive index, globular size, zeta potential, polydispersity index, ginger extract content. The formulation F1 showed best physicochemical properties with smallest globular size. It also showed significant (p<0.05) anti-inflammatory effect as compared to reference piroxicam drug solution. Based on the results, it is concluded that ginger extract can be used to develop stable microemulsion system and promising anti-inflammatory activity.

Mini Review: Chronic obstructive pulmonary disease, its new drug treatments and strategies: A review.

COPD is a complicated disease. Current available treatments are just for symptomatic relief and they cannot reverse the damages to lungs tissues due to alveolar destruction in COPD. Research is being conducted to evaluate new treatments and strategies to find specific treatments to minimize the symptoms of COPD. A new mixture of herbal medicine i.e AKL1 has emerged and thought to cure COPD symptoms especially cough related quality of life of COPD patients. Although, the results have showed no significant difference as compared to placebo but researchers recommend further evaluation in a large population (COPD Patients) group. Another medicine Roflumilast, a phosphodiesterase 4 inhibitor, was also found to be effective to treat COPD under specific recommendations with further research needed. Finally another medicine Indacaterol, a novel, once-daily (o.d) inhaled long-acting ß2-agonist proved to be effective clinically to treat COPD related broncho-constriction and also increasing the COPD patient's compliance by reducing the number of doses as compared to other conventional inhaled bronchodilators such as Albuterol.

Dengue fever: natural management.

Dengue fever is caused by the mosquito-borne dengue virus (DENV) serotypes 1-4, and is the most common arboviral infection of humans in subtropical and tropical regions of the world. Dengue virus infections can present with a spacious range of clinical signs, from a mild feverish illness to a life-threatening shock syndrome. Till now, there is no approved vaccine or drug against this virus. Therefore, there is an urgent need of development of alternative solutions for dengue. Several plant species have been reported with anti-dengue activity. Many herbal/natural drugs, most of which are commonly used as nutritional components, have been used as antiviral, larvicidal, mosquitocidal and mosquito repellents that may be used against dengue. The objective of this review article was to provide current approaches for the treatment and management/prevention of dengue fever by targeting viral proteins involved in replication cycle of the virus and different developmental stages of mosquito.

Whitening efficacy of plant extracts including Hippophae rhamnoides and Cassia fistula extracts on the skin of Asian patients with melasma.

INTRODUCTION: Melasma/hyperpigmentation and solar damage of the skin remains a difficult problem to treat. Various types of whitening agents are used to treat hyperpigmentation. A change has been observed recently to use plant extracts as skin whitening agents. AIM: To compare the effectiveness of emulsion formulations containing plant extracts that include catechins/polyphenols and placebo without plant extracts, on patients with melasma. MATERIAL AND METHODS: Two groups of 25 patients each (aged 21-35 years), who reported to the outpatient department of BV Hospital and Personal clinic of a dermatologist, were included in the study. Volunteers applied the formulations with plant extracts and placebo to one side of the cheek. Prior to the study, signed consent was obtained from each patient. The tyrosinase inhibitory activity of the extracts and formulations was tested in vitro. The pigment density of patients was evaluated biometrologically using Mexameter(®) and subjectively using a visual survey before and after treatment of 12 weeks. The approval of the Institutional Ethics Committee of Faculty of Pharmacy, the Islamia University of Bahawalpur was obtained before the study. One-way ANOVA and Kruskal-Wallis tests were used in the statistical analysis. RESULTS: A significant decrease in the level of melanin was determined in all 50 patients who used a plant extract containing catechin (p ≤ 0.05). The difference between pre- and post-treatment levels of melanin was statistically significant (p = 0.05). Formulations prepared with plant extracts containing catechin were found effective on melasma, compared to the placebo. CONCLUSIONS: Formulations containing plant extracts that are not yet being used widespread commercially on melasma could be an effective alternative treatment of melasma.

Fabrication, physicochemical characterization and preliminary efficacy evaluation of a W/O/W multiple emulsion loaded with 5% green tea extract

Complex multiple emulsions have an excellent ability to fill large volumes of functional cosmetic agents. This study was aimed to encapsulate large volume of green tea in classical multiple emulsion and to compare its stability with a multiple emulsion without green tea extract. Multiple emulsions were developed using Cetyl dimethicone copolyol as lipophilic emulsifier and classic polysorbate-80 as hydrophilic emulsifier. Multiple emulsions were evaluated for various physicochemical aspects like conductivity, pH, microscopic analysis, rheology and these characteristics were followed for a period of 30 days in different storage conditions. In vitro and in vivo skin protection tests were also performed for both kinds of multiple emulsions i.e. with active (MeA) and without active (MeB). Both formulations showed comparable characteristics regarding various physicochemical characteristics in different storage conditions. Rheological analysis showed that formulations showed pseudo plastic behavior upon continuous shear stress. Results of in vitro and in vivo skin protection data have revealed that the active formulation has comparable skin protection effects to that of control formulation. It was presumed that stable multiple emulsions could be a promising choice for topical application of green tea but multiple emulsions presented in this study need improvement in the formula, concluded on the basis of pH, conductivity and apparent viscosity data.

Emulsões múltiplas complexas possuem excelente habilidade de agregar grandes quantidades de agentes cosméticos funcionais. Este estudo teve por objetivo encapsular grandes volumes de chá verde em uma emulsão múltipla clássica e comparar sua estabilidade com a emulsão múltipla sem o extrato do chá verde. Emulsões múltiplas são desenvolvidas usando cetil dimeticona copoliol como emulsificante lipofílico e o clássico polissorbato-80 como emulsificante hidrofílico. As emulsões múltiplas foram avaliadas por meio de vários aspectos fisico-químicos como condutividade, pH, análise microscópica e reologia. Estas características foram observadas por um período de 30 dias sob diferentes condições de armazenamento. Testes de proteção da pele in vivo e in vitro foram realizados para ambos os tipos de emulsões testadas, i.e. com o ativo em estudo (MeA) e sem ativo (MeB). Ambas as formulações apresentaram características comparáveis no que diz respeito aos diferentes fatores físico-químicos avaliados sob diferentes condições de armazenamento. A análise reológica mostrou que as formulações apresentaram comportamento pseudo-plástico sob contínuo estresse de cisalhamento. Os resultados dos testes in vivo e in vitro sobre a proteção da pele revelaram que a formulação ativa promoveu efeitos comparáveis à formulação controle. Nossos dados mostraram que emulsões múltiplas estáveis poderiam ser escolhas promissoras para a aplicação tópica do chá verde. Entretanto, a fórmula das emulsões múltiplas apresentadas neste estudo precisam ser melhoradas no que diz respeito ao pH, condutividade e viscosidade aparente.

Formulation and characterization of a cream containing extract of fenugreek seeds.

Fenugreek seeds possess antioxidant effects and contain a mucilage which has emollient properties. It can also produce skin healing, whitening, moisturizing, skin soothening and antiwrinkle effects. The purpose of study was to formulate a stable W/O emulsion containing fenugreek seeds extract using liquid paraffin oil. Fenugreek seeds extract, which was obtained by concentrating methanolic extract of fenugreek seeds, was entrapped in the inner aqueous phase of W/O emulsion. A base containing no active material and a formulation containing concentrated extract of fenugreek (in a concentration of 4%) in the internal aqueous phase (W/O emulsion) were prepared and stored at different accelerated conditions for a period of four weeks to predict the stability of these creams. It was found that both, the base and the formulation, were stable at all the accelerated conditions regarding color, liquifaction and phase separation. However, insignificant changes in the pH of base and significant changes in the pH of the formulation were observed with the passage of time. Both the base and the formulation were applied to the cheeks of human volunteers for six weeks and various parameters of the skin were evaluated every week to measure any effect produced by these creams. All the effects of base were statistically significant except the sebum contents and pH, which changed but insignificantly. A significant decrease on skin melanin and erythma was produced by the formulation. An insignificant decrease in TEWL was observed for the formulation.