Evaluation of Plantago major L. seed mucilage as a rate controlling matrix for sustained release of propranolol hydrochloride

Polysaccharide mucilage derived from the seeds of Plantago major L. (family Plantaginaceae) was investigated for use in matrix formulations containing propranolol hydrochloride. HPMC K4M and tragacanth were used as standard for comparison. The hardness, tensile strength, and friability of tablets increased as the concentration of mucilage increased, indicating a good compactibility of the mucilage powders. The rate of release of propranolol hydrochloride from P. major mucilage matrices was mainly controlled by the drug/mucilage ratio. Formulations containing P. major mucilage were found to exhibit release rate comparable with HPMC containing matrices at a lower drug/polymer (drug/HPMC 2:1). These results demonstrated that P. major mucilage is a better release retardant compared to tragacanth at equivalent content. The results of kinetic analysis showed that in F3 (containing 1:2 drug/mucilage) the highest correlation coefficient was achieved with the zero order model. The swelling and erosion studies revealed that, as the proportion of mucilage in tablets was increased, there was a corresponding increase in percent swelling and a decrease in percent erosion of tablets. The DSC and FT-IR studies showed that no formation of complex between the drug and mucilage or changes in crystallinity of the drug was occurred

Topical gel of Metformin solid lipid nanoparticles: a hopeful promise as a dermal delivery system

The aim of the present study was to enhance the skin delivery of metformin by making solid lipid nanoparticles containing metformin using the ultra-sonication method. To achieve the optimum skin delivery for metformin, the effects of the ratio of two surfactants (Tween:Span) on nanoparticles properties and their performance were investigated. Photon correlation spectroscopy, scanning electron microscopy (SEM), Powder X-ray Diffractometer (PXRD), Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were used to characterize the solid state of metformin in solid lipid nanoparticles. Generally, the particle size of nanoparticles decreased by the addition of co-emulsifier (Span®60). Results showed that all formulations made by binary mixtures of surfactants had low particle size, low Polydispersity index and high zeta potential. It was interesting to note that the smallest nanoparticles (203.8 ± 15.356) was obtained when the HLB of the binary surfactants (HLB of 11.67) was closer to the HLB of beeswax (HLB of 12) used in the preparation of SLN. It was also found that by decreasing the HLB of the system from 14.9 to 10.06 the zeta potential of SLNs increased from −0.651 ± 0.315 to −6.18 ± 0.438 mV. But, a further reduction in the HLB from 10.06 to 8.45 caused a reduction in the zeta potential from −6.18 to −3.596 ± 0.255. Results showed that the highest entrapment efficiency of 45.98 ± 9.20% was obtained for formulation with larger particle size and with the highest HLB value (HLB 14.9). DSC study showed that metformin in SLN is in an amorphous form. FT-IR spectra of Met-SLN showed that the prominent functional groups existed in the formulations which could be an indication of good entrapment of metformin in a lipid matrix. FT-IR results also ruled out any chemical interaction between the drug and the excipients. The amounts of metformin detected in the skin layers and the receptor chamber at all sampling times were higher for nanogel compared to metformin gel. This is an indication of a better performance of Metformin nanogel ex-vivo and could be developed further for clinical studies

Formulation and Evaluation of Rose Oil Nanoemulsion %0.1 on Skin Properties

Introduction: One of the causes of the skin drying is lack of oil secretion by sebaceous glands in skin. Then this can make skin sensitive to environmental factors and some substances. Ancient Iranians have used rose water for washing the face and increase moister of skin. Nano-emulgel Due to its high stability, biocompatibility and proper solubility in water are considered as good carriers for targeted drug delivery, and have a good potential for drug delivery because they have the properties of nanoparticles of colloids and hydrogels simultaneously. In this research, effects of rose oil nanoemulgel %0.1 are evaluated on the normal and dried skin. Methods and Results: Different formulations of rose oil were evaluated using suitable surfactants. Then the best ratio of nano-emulgel Red flowers and sustainability criteria were determined. Rose oil components were identified by GC/MS. Clinical studies were conducted for an eight-week on 60 healthy volunteers in two groups. A nano-emulgel %0.1 rose oils and other non-essential emulgel with the same basic materials were used and the amount of sebum secretion, melanin, skin redness, hydration and elasticity of the skin and also complications were determined. Quantitative data analysis was done by using Chi-square test and P≤0.05 were considered significant. The results have demonstrated the effectiveness of the rose oils in skin hydration. Two groups with other characteristics such as the skin secretion of sebum, elasticity, pigmentation , and redness have shown similar effects. However, both groups did not show any complications. Conclusions: In this study, the main ingredient of essential oil is alcohol. The most important terpene alcohols are, 31% Nonadecane, 38% Citronellol, 23% Linalool , and 17% Heneicosane. The good effectiveness of Rose oil on increasing of skin moisture is the appropriate treatment of skin drying

Evaluation of binding properties of Plantago psyllium seed mucilage.

Pharmaceutical ingredients are required in the preparation of a drug tablet: fillers to increase the bulk and lubricants to reduce friction during the tableting process. Some pharmaceutical ingredients require a binder for tableting. This provides the cohesiveness necessary for binding ingredient granules under compression. The quantity used must be carefully regulated, since the tablet must disintegrate after administration to liberate the drug (1). Binders act by causing aggregation of powders, thereby forming granules through the granulation process. They modify the cohesive properties of the granules by promoting the formation of strong cohesive bonds between such particles (2). Mucilages and gums are well known for their medicinal use. In recent times, increasing attention has been given to the application of gums of various sources as phar- Mucilage extracted from Plantago psyllium seeds was evaluated for inertness and safety parameters. The suitability of psyllium mucilage for a pharmaceutical binder was assessed in paracetamol tablets. Properties of the granules prepared using different concentrations of psyllium mucilage was compared with PVP and tragacanth. Psyllium mucilage at 5 % (m/m) was found to be comparable with 3 % (m/m) of PVP. Investigated paracetamol tablets indicated that psyllium mucilage can retard the drug release

An investigation on parameters affecting the optimization of testosterone enanthate loaded solid nanoparticles for enhanced transdermal delivery

The current research aimed to formulate and optimize testosterone enanthate-loaded solid lipid nanoparticles (TE-SLNs) for the enhanced TE transdermal delivery. To this end, TE-SLNs were prepared using ultrasound-assisted emulsification technique and their properties and permeation across the excised rat skin were investigated. Evaluation of lipid type as well as the ratio and contents of surfactant mixtures resulted in a polydispersity index, particle size, drug loading, drug encapsulation efficiency, and zeta potential of 0.317 ± 0.006, 87.66 ± 1.52 nm, 21.61 ± 0.45 %, 44.71 ± 1.14 % and -23.06 ± 0.50 mV, respectively. ATR-FTIR spectra of TE-SLNs exhibited the prominent functional groups of TE in the formulations, indicating a well-dispersion of TE in the lipid matrix without any chemical interaction with other components of the formulation. Differential scanning calorimetry (DSC) demonstrated that TE in SLNs is in an amorphous state. Transmission electron microscopy (TEM) confirmed that the prepared TE-SLNs have a stable size and maintained their sphericity. The results of TE permeation across the excised rat skin from SLNs displayed cumulative amounts of 110.61 ± 17.7 µg/cm2, which is 3.2 fold improvement in TE permeation in comparison with the testosterone enanthate solution in oleic acid (p < 0.05). Furthermore, no cellular toxicity was observed for the nanoparticles. The results showed that the prepared TE-SLNs can be applied as the potential carriers for transdermal delivery of testosterone enanthate

Spironolactone loaded nanostructured lipid carrier gel for effective treatment of mild and moderate acne vulgaris: a randomized, double-blind, prospective trial

Spironolactone (SP) known as an anti-androgen drug, has been proven to be effective in treatment of acne. The quest to minimize the unnecessary systemic side effects associated with the oral drug administration of spironolactone, has led to a growing interest of loading SP on lipid nanoparticles to deliver the drug in a topical formulation. The aim of the current investigation was to prepare and compare the performance of SP loaded nanostructured lipid carrier (SP-NLC) and SP alcoholic gels (SP-ALC) on two groups of respective patient populations, group A and group B in the treatment of mild to moderate acne vulgaris. The results showed that SPNLCs were spherical in shape with an average diameter of ~240 nm. The polydispersity index (PI) and zeta potential of these nanoparticles were 0.286 and -21.4 respectively. The gels showed non-Newtonian independent pseudoplastic and shear thinning behavior. The SP-NLCs was not toxic to fibroblast cell strains at the 24 and 48 h periods. Results showed that the mean number of total lesions (37.66 ± 9.27) and non-inflammatory lesions (29.26 ± 7.99) in group A significantly decreased to 20.31 ± 6.58 (p<0.05) and to 13.95 ± 5.22 (p<0.05) respectively. A similar pattern was observed for group B where the mean number of total lesions and non-inflammatory lesions reduced from 33.73 ± 9.40 to 19.13 ± 5.53 (p<0.05) and from 25.65±8.12 to 13.45 ± 4.48 (p<0.05) respectively. The total lesion count (TLC) was significantly decreased from 37.16 ± 9.28 to 19.63 ± 6.36 (for group A; p<0.071) and 32.60 ± 9.32 to 18.33 ± 5.55 (for group B; p<0.05) respectively. After treatment with SP-NLC for 8 weeks, the water content of the skin significantly (p<0.05) increased from 37.44 ± 8.85 to 45.69 ± 19.34 instrumental units. Therefore, the SP-NLC gel may help in controlling acne vulgaris with skin care benefits

Development of a novel nanoemulgel formulation containing cumin essential oil as skin permeation enhancer

Essential oils have been proposed as promising non-toxic transdermal permeation enhancers. Their use is limited because of their low water solubility. The use of nanotechnology-based strategies is one of the ways to overcome this limitation. This study aimed to explore the transdermal permeation enhancing capability of cumin essential oil in nanoemulgel systems containing diclofenac sodium. Cumin essential oil nanoemulsion was produced by high-pressure homogenization technique. The formulation was optimized by changing HLB values in a range of 9.65–16.7 using different surfactant mixtures, namely, Tween 20, Tween 80, and Span 80. Preparations were characterized by polydispersity index, droplet size, and zeta potential. Nanoemulsion with concentrations of 2 and 4% essential oil was incorporated into 0.75% Carbopol gel matrix to make nanoemulgel formulation, and its permeation enhancing effect was performed through Franz diffusion cells. Antinociceptive activities of the formulations were measured in thermal (tail-flick) and chemical (formalin) models of nociception in mice. Characterization exhibited that at HLB value of 9.65, the smallest particle size (82.20 ± 5.82 nm) was formed. By increasing the essential oil percentage in the nanoemulgel from 1 to 2%, the permeation of diclofenac increased from 28.39 ± 1.23 to 34.75 ± 1.07 µg/cm2 at 24 h. The value of permeation from the simple gel (21.18 ± 2.51 µg/cm2) and the marketed product (22.97 ± 1.92 µg/cm2) was lower than the formulations containing essential oil. Nanoemulgel of diclofenac containing essential oil showed stronger antinociceptive effects in formalin and tail-flick tests than simple diclofenac gel and marketed formulation. In conclusion, the study proved that nanoemulgel formulation containing cumin essential oil could be considered as a promising skin enhancer to enhance the therapeutic effect of drugs. Graphical abstract: [Figure not available: see fulltext.]

Improved yeast delivery of fluconazole with a nanostructured lipid carrier system

Despite the growing trends in the number of patients at risk for invasive fungal infections, management with current antifungal agents results in complications due to changes in the epidemiology and drug susceptibility of invasive fungal infections. In the present research fluconazole-loaded nanostructured lipid carriers were prepared using probe ultrasonication techniques and investigated the efficacy of the optimal formulation on a large number of Candida species. The morphology of the obtained nanostructured lipid carriers was characterized by transmission-electron microscopy. The minimum inhibitory concentrations (MIC) for the new formulations against strains of Candida were investigated using the Clinical and Laboratory Standards Institute document M27-A3 and M27-S4 as a guideline. The fluconazole-loaded nanostructured lipid carriers presented a spherical shape with a mean diameter, zeta potential and entrapment efficiency of 126.4 ± 15.2 nm, −35.1 ± 3.0 mV, and 93.6 ± 3.5%, respectively. The drug release from fluconazole-loaded nanostructured lipid carriers exhibited burst-release behavior at the initial stage followed by sustained release over 24 h. Using a new formulation of fluconazole led to a significant decrease in MICs for all Candida groups (P < 0.05). Furthermore, C. albicans isolates showed more susceptibility to fluconazole-loaded nanostructured lipid carriers than C. glabrata and C. parapsilosis (P < 0.05). The MIC50 drug concentration was obtained as 0.0625, 0.031 and 0.25 μg/ml for fluconazole-resistant strains of C. albicans, C. glabrata, and C. parapsilosis, respectively. In conclusion, a novel delivery system which can be used as part of a strategy to improve the antifungal activity of fluconazole against various Candida strains with different susceptibilities to conventional formulations of fluconazole was evaluated

Preparation and In-Vitro Evaluation of Ketoconazole-Loaded Niosome (Ketosome) for Drug Delivery to Cutaneous Candidiasis

Background: Recently, niosomes are becoming popular in drug delivery. The current work aimed to investigate the characteristics, cellular safety, and antifungal activity of ketoconazole-loaded niosome (ketosome). Methods: Ultrasonic approach was employed to prepare ketosome including cholesterol, nonionic surfactant and ketoconazole. The size characteristics and morphological features of ketosome and physicochemical properties of ketoconazole in ketosomes were evaluated using dynamic light scattering (DLS), differential scanning calorimetry (DSC), powder x-ray diffractometer (PXRD), scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy. Also, the dissolution rate, cellular safety test and antimycotic properties of ketosome were examined. Results: According to the results, the particle size of the ketosome decreased from 491.400±10.622 to 121.300±7.274 nm by the increment of cholesterol. According to further research, changes in the cholesterol:surfactants ratio can modulate the zeta potential from -27.866±1.069 to -12.500±1.153 mV. The highest entrapment of ketoconazole was about 87% when the cholesterol concentration in the ketosome was high. Ketosome with the maximum cholesterol:surfactants ratio showed the fastest drug release. Furthermore, the cell viability assay revealed that the ketosome had lower cytotoxicity in comparison with pure drug. The cell viability of the ketosome was estimated to be about 90% (HGF cell line). The ketosome had a lower MIC than the pure drug when tested against Candida albicans. Conclusion: The results of this study revealed that the optimized ketoconazole-loaded niosome could be used as a possible nanovesicle for ketoconazole drug delivery, potentially opening up new ways for the management of cutaneous candidiasis complaints