Semisolid Formulations Research Articles

SOME PHYSICOCHEMICAL PROPERTIES OF GEORGIAN BENTONITE CLAY

Clay minerals are known as biocompatible materials and have been utilized for medicinal aims from long ago. Currently, bentonite clays have also been widely investigated for broad spectrum of new applications in many biomedical spheres due to their unique properties - expansion and adsorption abilities - which are very useful in pharmaceutics, cosmetics, drug delivery systems and tissue engineering. Swelling has a significant impact on the rheological and physical properties of clay. It depends on many factors including temperature, pH, and polarity. In addition, since bentonites have negative surface charge they possess high adsorption ability for cationic elements. The priority task at the I. Kutateladze Institute of Pharmacochemistry TSMU is to extend the biopharmaceutical application of Georgian bentonite clay. Several semisolid formulations were proposed on the bases of the preparation - Tikha Ascane (TA), received from the clay of Askana Deposit (Ozurgeti region of Georgia). In this study we investigated the swelling capability of TA in the presence of different temperatures, polarities and pH; the interaction behaviour of bentonite with cationic compounds was also evaluated. As many researches are focused on the combination clay minerals with cationic polymers for the preparation of effective therapeutic systems, we examined the suitability of TA as a substrate for the obtaining hybrid composites with biopolymer Chitosan (CS). The samples were characterized by examining FTIR spectra and morphology. The obtained data indicate that swelling capability of TA is affected by temperature, pH, and polarity of solutions.  FTIR analysis showed that cationic drug and polymer (CS) can be successfully incorporated in TA through adsorption and formation chemical bonds. Microscopic analyses demonstrated homogeneity of TA-CS composites. These results will be used in future for preparing drug - clay or drug - polymer composites based on TA for biomedical application.

Investigation of The Effect of Semi-Solid Temperatures and Holding Times at Isothermal Range On Microstructure of AZ31 Mg Alloy

Mg alloys have poor formability due to their hexagonal tightly packed (HCP) crystal structure, low active shear system at room temperature, and anisotropic behavior in polycrystalline structure. While this situation hindered the development and commercialization of Mg alloys to some extent in the past, today developments in machining, liquid forming and semi-solid forming technology have removed these obstacles. Semi-solid forming of alloys has been the subject of intense R&D since it was discovered in the 1970s. In the semi-solid forming method, it is aimed to obtain ideal microstructure of the alloy, including excellent fluidity, appropriate flow control, adjustable viscosity and controllable grain morphology, thanks to equiaxed spherical solid particles surrounded by liquid. In this study, it is aimed to achieve the spherical microstructure required for the semi-solid shaping of the extruded AZ31 Mg alloy by heating to semi-solid temperatures and isothermal holding in the semi-solid temperature range. To accomplish this objective, rapid heating in the induction coil and controlled holding in the isothermal temperature range were applied to the alloy. Heating the extruded AZ31 Mg alloy to a semi-solid temperature (565-630°C) and subsequently rapid cooling processes lead to many intermetallic Mg17Al12(γ) compounds with heterogeneous distribution both in the equiaxed primary Mg(α) grains and at the grain boundaries as well as a very little eutectic at the grain boundaries. As the semi-solid temperature value increased, the degree of spheroidization increased. However, it was found that the grain growth reached a maximum at one point and there was no significant change in the shape factor as a result of controlled holding time.

Thermosensitive TMPO-oxidized lignocellulose/cationic agarose hydrogel loaded with deferasirox nanoparticles for photothermal therapy in melanoma

Deferasirox (DFX) is an iron-chelating agent effective in treating various kinds of cancers, which inhibits iron metabolism in cancer cells. The recent study aimed to prepare an injectable thermosensitive hydrogel based on lignocellulose and agarose containing deferasirox-loaded polypyrrole nanoparticles for local drug delivery in a combined chemo-photothermal therapy by laser light irradiation. Polypyrrole nanoparticles containing DFX were made by the emulsification method and optimized. Thermosensitive hydrogels were prepared by quaternary ammonium substituted agarose and TMPO-oxidized lignocellulose at different ratios, and the optimal hydrogel was selected based on gelation time, gelation temperature, and injectability. DFX- loaded polypyrrole nanoparticles were then added to the hydrogel, and the drug release, rheology test, injectability, degradation, and swelling percent, as well as cytotoxicity, and photothermal properties, were studied on B16F10, human melanoma cells. The hydrogel with 2 % anionic lignocellulose and 0.5 % cationic agarose showed the shortest gelation time and the highest mechanical strength. It transferred from a liquid state at 4 °C into a semisolid form at 37 °C with a gelation time of 10.3 min. The nanoparticles loaded in hydrogel showed dose-dependent cytotoxicity. The cytotoxic dose of the drug was reduced by laser light irradiation.

Terbinafine HCl Film-Forming Spray for the Treatment of Topical Fungal Infections

Abstract: Terbinafine HCl is an allylamine used to treat fungal infections. It has substantial side effects that can be mitigated by using a topical semisolid dose form. The objective of this study was to develop a 1% Terbinafine HCl film-forming spray formulation to treat topical fungal infections. The formulation was developed by combining polymers, penetration enhancer, plasticizer, and a suitable solvent system. The central composite design with 3 independent variables and 2 dependent variables is implemented to optimize the formulation. The film-forming spray was put through its tests to assess formulation and container-related parameters such as pH, spray angle, spray pattern, density, volume delivered for one actuation and evaporation time. From the study, it was observed that the concentration of ethyl cellulose and Eudragit RSPO has a greater influence on the viscosity of the spray solution, whereas the eutectic mixture has a greater influence on the drug permeation followed by the polymers. It also tested with various fungi, and it was found that formulation showed better fungicidal activity than the marketed product achieved by triple action. The stability studies have shown that the optimized formulation was stable with temperature of 25 ± 2°C and RH 60 ± 5(six months) on the pH, viscosity and visual appearance of the formulation. The study has concluded that the formulated film-forming spray formulation is highly efficient in treating topical and transdermal fungal infections when compared to the traditional dosage forms. Keywords: Terbinafine HCl, Formulation, Fungal infection, Solid dosage forms, Ethyl cellulose.

A rapid HPTLC method to estimate ximenynic acid in semisolid dosage formulation

A novel HPTLC analytical technique and validation study were developed to determine the concentration of ximenynic acid (XMA) in semisolid dosage formulations (SDF) such as cream, gel, lotion, etc. The procedure makes use of reverse-phase high-performance liquid chromatography (HPLC). This study presents the first report of sensitive, selective, precise and robust HPTLC method, which has been developed and validated for quantification of the XMA from pharmaceutical formulation. The chromatographic development was carried out on HPTLC plates precoated with silica gel 60 F254 using a mixture of Toluene: Ethyl Acetate: Methanol: Formic acid (5:4:0.5:0.5 v/v/v/v) as mobile phase. Detection was carried out densitometrically at 254 nm. The Rf value of XMA were found at Rf about 0.3 ± 0.01. The method was validated as per ICH guideline with respect to linearity, accuracy, precision, robustness etc. The method is new, simple and economic for routine estimation of XMA in bulk, preformulation studies and pharmaceutical formulation to help the industries as well as researchers for their sensitive determination of XMA rapidly at low cost in routine analysis. Because XMA has the potential to be a game-changing method of treating ageing, its advancement may benefit the pharmaceutical and cosmetics sectors. Ximenynic acid; Skin Care Medicinal Formulation; HPTLC; Validation

Development and validation of HPLC method for ximenynic acid in semisolid dosage formulation

A novel analytical technique and validation study were developed to determine the concentration of ximenynic acid (XMA) in semisolid dosage formulations (SDF) such as cream, gel, lotion, etc. The procedure makes use of reverse-phase high-performance liquid chromatography (HPLC). A Phenomenex Luna Column 5 (4.6 x 250 mm) was used for the analysis, using acetonitrile as the mobile phase, sodium dihydrogen phosphate monohydrate as the stationary phase, and 229 nm detection at 30 degrees Celsius. In spite of the presence of additional compounds, their presence had no effect on the detection of XMA in SDF. As part of validating this HPLC technique, a number of tests were performed to evaluate its specificity, linearity, accuracy, precision, and durability. International Conference on Harmonization standards were used to determine whether the method was adequate (ICH). Because it is simple to implement and produces reproducible results, the presented HPLC approach has the potential to be utilized in industry to standardize herbs and Phytomedicines. Because XMA has the potential to be a game-changing method of treating ageing, its advancement may benefit the pharmaceutical and cosmetics sectors.

The challenge of improving pterostilbene (PTS) solubility for solid and semi-solid dosage forms: The obtention of binary and ternary systems

Pterostilbene (PTS) is a drug candidate with low water solubility and poor bioavailability. On the other hand, drug:cyclodextrins complexes frequently provide bulk powders with low drug concentrations, which is crucial for obtention solid or semi-solid pharmaceutical dosage forms. In order to determine the optimal conditions for enhancing the solubility of PTS:BCD (β-cyclodextrin) complex, a Box–Behnken design was performed. Although the optimal conditions have been applied, low complexation efficiency (0.127) and the bulk powder remained. A PTS:BCD:HPMC (HPMC, hydroxypropyl methylcellulose) ternary system was developed to overcome this limitation, comparing two media, water and a mixture of ethanol–water. When ethanol was used as a co-solvent, the PTS:BCD:HPMC ternary system (freeze-dried) contained 116.65 ± 1.40 mg/g of PTS. This value was 3.4-fold higher than the PTS content observed when the same ternary system was obtained in aqueous media (34.8 mg/g) and 2.8-fold higher than the PTS content observed for PTS:BCD complex (freeze-dried) obtained using ethanol as a co-solvent. Dissolution tests revealed that after 120 min, in a buffer with a pH value of 1.2, only 43% of PTS dissolved. In contrast, 80% and 90% of PTS were dissolved from the PTS:BCD complex and PTS:BCD:HPMC ternary system, respectively. Moreover, the dissolution was fast in a buffer with a pH value of 6.8. PTS:BCD complex reached the maximum PTS dissolution at 75 min and PTS:BCD:HPMC at 45 min. In summary, the results of this study demonstrated, for the first time, that low-bulk powders with a high content of PTS can be obtained from PTS:BCD:HPMC ternary systems using ethanol as a co-solvent. This new finding offers a valuable alternative for producing solid or semi-solid formulations containing highly soluble PTS.

Ethosomal Gel for Topical Administration of Dimethyl Fumarate in the Treatment of HSV-1 Infections.

The infections caused by the HSV-1 virus induce lesions on the lips, mouth, face, and eye. In this study, an ethosome gel loaded with dimethyl fumarate was investigated as a possible approach to treat HSV-1 infections. A formulative study was conducted, evaluating the effect of drug concentration on size distribution and dimensional stability of ethosomes by photon correlation spectroscopy. Ethosome morphology was investigated by cryogenic transmission electron microscopy, while the interaction between dimethyl fumarate and vesicles, and the drug entrapment capacity were respectively evaluated by FTIR and HPLC. To favor the topical application of ethosomes on mucosa and skin, different semisolid forms, based on xanthan gum or poloxamer 407, were designed and compared for spreadability and leakage. Dimethyl fumarate release and diffusion kinetics were evaluated in vitro by Franz cells. The antiviral activity against HSV-1 was tested by plaque reduction assay in Vero and HRPE monolayer cells, while skin irritation effect was evaluated by patch test on 20 healthy volunteers. The lower drug concentration was selected, resulting in smaller and longer stable vesicles, mainly characterized by a multilamellar organization. Dimethyl fumarate entrapment in ethosome was 91% w/w, suggesting an almost total recovery of the drug in the lipid phase. Xanthan gum 0.5%, selected to thicken the ethosome dispersion, allowed to control drug release and diffusion. The antiviral effect of dimethyl fumarate loaded in ethosome gel was demonstrated by a reduction in viral growth both 1 h and 4 h post-infection. Moreover, the patch test demonstrated the safety of the ethosomal gel applied on the skin.

The substantiation of the composition of a soft medicine for the therapy of inflammatory diseases of the musculoskeletal system

Aim. To substantiate the optimal composition of the base of the semisolid dosage form with the thick extract of feverfew (Tanacetum parthebased on structural-mechanical, textural, adhesive and microscopic studies. Materials and methods. The study objects were samples of a semisolid dosage form with the thick extract of feverfew with various gelling agents and the reference drug “Irikar”. In the course of the research, a complex of structural-mechanical methods and the microscopic analysis of the samples were used. Results and discussion. The studies of structural-mechanical properties have determined the regularities in the rheological characteristics of the experimental samples made using different gelling agents. It has been found that the rheogram of the emulgel sample has a smooth transition from the elastic deformation region to the elastic-plastic one, which may indicate a more homogeneous distribution of the sample components. It has been also determined that the sample corresponds in the textural properties to the refenium) rence drug – “Irikar” cream. The structural-mechanical studies have substantiated the rational content of the gelling agent in the emulgel composition – 3 %. The results of rheological studies have been confirmed by the data of the microscopic studies. Conclusions. The data obtained are the basis for further pharmaceutical development of a drug with the thick extract of Tanacetum parthenium for the treatment of diseases of the musculoskeletal system.

Influence of Technological Parameters on the Size of Benzocaine Particles in Ointments Formulated on Selected Bases

Compounding formulations, including semi-solid medication forms, must meet criteria related to specific stability and quality, during a period of their use. In suspension-type ointments, one of the criteria for assessment of their correct manufacturing is particle size, which in the compounding preparation cannot exceed 90 µm. An appropriate level of particle disintegration can be achieved via a selection of technological parameters and qualitatively compatible excipients. In this study, benzocaine ointments were prepared using a levigation process. The time of its application on the particle size of API in suspension ointments was evaluated. In parallel, the effect of mixing parameters and the co-solvent used on the precipitation of active substance crystals in emulsion ointments during the storage of these formulations for 28 days was investigated. Forty suspension and emulsion ointments were prepared using selected ointment bases: Pentravan®, Lekobaza, Lekobaza LUX, Eucerin Ointment I, Nourivan™ Antiox, Fitalite™, containing 2% benzocaine. Based on the results of the stability test, four formulations were selected to study the release kinetics of benzocaine in vitro. These formulations were characterized by the rate of release consistent with the Higuchi model, and the fastest rate of release occurred from the Eucerin-based emulsion ointment.

Phytochemical profile, in vitro activities, and toxicity of optimized Eugenia uniflora extracts

In this study, we investigated the influence of mixture design on the chemical profile of Eugenia unifloraleaves, evaluating the antioxidant and antimicrobial activities, the toxic and hemolytic potential, with the focus on the improvement of the polyphenol’s extraction for incorporation of the extract in semi-solid forms with antifungal action. The chemical analysis was evaluated by UV-Vis and HPLC. The antimicrobial, antioxidant, and hemolytic activities were monitored. The flavonoid content ranged from 2.63-7.98 %w/w and tannins from 5.42-18.29 %w/w. The extract consisted of gallic acid (0.09-1.29%; w/w), ellagic acid (0.09-0.37%; w/w), and myricitrin (0.18-1.20%; w/w). The most successful solvent system with the highest level of active extract was water: ethanol: propylene glycol. The extracts showed fungicidal properties (3.9 μg/mL), high antioxidant activity (IC50: 9.50 μg/mL), and low toxicity. These solvent mixtures can improve the in vitro bioactivities when compared to pure solvents and this result demonstrates the importance of mixture designs as useful tools for creating high-quality herbal products and elucidate the potential of E. unifloraglycolic extracts as active herbal pharmaceutical ingredients in topical delivery systems.

FORMULATION AND IN VITRO EVALUATION OF A NOVEL MEFENAMIC ACID TOPICAL CREAM

Mefenamic acid (MA) is a Non-Steroidal Anti-Inflammatory Drug (NSAID), which has been established in pharmacologic management of musculoskeletal disorders. This study was designed to formulate and conduct an in vitro evaluation of a novel MA topical cream, which would reduce the gastrointestinal associated toxicities related to oral administration. A concentration of 1-2% of MA was prepared by using a different combination of the excipients. Either ethanol or dimethyl sulfoxide (DMSO) are employed as vehicles for hydrophobic compounds, which are commonly used as solvents. The creams were evaluated by their physical properties, stability studies and addition of an in vitro anti-inflammatory test for mefenamic acid creams. The physical studies include organoleptic test, pH test, spreadability test and dye test while for the stability studies, the creams were tested with accelerated stability studies and microbial growth. MA in DMSO showed better anti-inflammatory effect compared to MA in ethanol in the correlation of results with that of marketed products. In conclusion, this study proved that MA cream can also be a good choice of semi-solid formulation and further studies would be suggested to enhance this cream as a novel choice of formulation to be introduced and marketed by the pharmaceutical industry

FORMULATION AND ASSESSMENT OF CLAY - POLYMER HYDROGEL BASED ON GEORGIAN BENTONITE

Bentonite clays are broadly employed in the design of varied drug delivery systems due to their characteristic feature such as adsorption, swelling ability and biocompatibility. Combination polymers with clay particles considerably improve mechanical and physical properties, drug - encapsulation efficiency and controlled release behavior of hybrids comparing with the starting components. One of the priority research areas at the I. Kutateladze Institute of Pharmacochemistry is extension the usage potential of Georgian bentonite clay in pharmacy, medicine, veterinary and cosmetics. Numerous semisolid dosage forms and dry ointments were proposed by the Institute on the bases of preparation Tikha Ascane, obtained from the clay of Askana Deposit (Ozurgeti region of Georgia).  The aim of this study was to examine the suitability of Tikha Ascane as a substrate for the obtaining hybrid material with Sodium alginate (SA) and develop and characterize drug loaded clay/ polymer hydrogel. Optimized formulation for Tikha Ascane/SA hybrids was selected and Nitrofurazone (NFZ) as a model drug was incorporated. The samples were characterized by examining FTIR spectra, morphology, viscosity, pH, homogeneity and appearance. Content of NFZ in hydrogel was determined by HPLC. FTIR analysis revealed that Tikha Ascane and SA act as a simply physical mixture. Infrared spectra showed that NFZ did not bind strongly to the hybrid material. Microscopic analyses allowed verification of homogeneity of samples. Optimal clay / polymer composites contained Tikha Ascane - SA at the ration of 1:3 (w/w) and 0.2 % w/w incorporated NFZ. From this work it is cleared that Georgian bentonite clay preparation - Tikha Ascane can be successfully used as a substrate for clay / polymer hybrid material; formulated complex exhibits promising characteristics that allows considering it as a potential drug delivery system. Further studies are on-going for the preparation of TA hybrid material with different polymers.

EVALUASI FISIK KRIM ANTIINFLAMASI EKSTRAK KULIT BAWANG MERAH DENGAN VARIASI KONSENTRASI TRIETANOLAMIN DAN ASAM STEARAT

Inflammation is the body's defense function against the entry of organisms and other disturbances. The drugs used often have an effect on gastrointestinal disorders, so other alternative treatments are being developed that can minimize side effects. The quarcetin content of shallot skin extract, which has anti-inflammatory activity, is formulated in a cream dosage form. The emulsifiers in the m/a cream formula are stearic acid and triethanolamine (TEA). This study aims to determine the physical evaluation of an anti-inflammatory cream containing shallot skin extract with variations in concentrations of TEA and stearic acid. The method used in this study is the experimental method. Formulations I, II, and III with varying concentrations of TEA and stearic acid (2:8%, 3:10%, and 4:12%) were used. Tests carried out included organoleptic tests, homogeneity, pH, spreadability, and adhesion. The cream formula passed the organoleptic test with a distinctive shallot smell, semi-solid form, brownish red color, all formulas were homogeneous, pH 5.264-6.417, spreadability 3.849-6.251 cm, and adhesion 83-132 seconds. Higher concentrations of TEA and stearic acid had an effect on adhesion and spreadability but had no effect on organoleptic properties, homogeneity, or pH. Onion skin extract cream with a concentration of TEA:2%:8% stearic acid gave the best physical quality.

Material characterization of GPX®: A versatile in situ solidifying embolic platform technology.

Endovascular embolization is a minimally invasive procedure during which blood flow to targeted tissues is selectively occluded. The list of clinical indications for embolization continues to expand. Liquid embolic agents are injectable compositions that transition into a solid or semi-solid form when introduced into blood vessels. The mechanism that triggers the liquid-to-solid transition is a key distinguishing feature of liquid embolic agents. GPX is a waterborne liquid embolic agent comprising oppositely charged polyelectrolytes: polyguanidinum and inorganic polyphoshate. In situ solidification is driven by electrostatic condensation of the polyelectrolytes, triggered by ionic strength differentials. We report in vitro characterization of the material properties of GPX, it is in vivo effectiveness in acute animal studies, and its potential for chemoembolization. The viscosity of GPX can be varied over a wide range by adjusting the polyguanidinium MW and/or concentration. Formulation of GPX with either tantalum microparticles (30wt%) or iodinated radiocontrast agents (300mgI ml-1) did not significantly change the flow behavior of GPX; the viscosity was independent of shear rate and remained within a clinically practical range (80-160cP). Formulation of GPX with doxorubicin substantially increased viscosity at low shear rates and resulted in a power law dependence on shear rate. High contrast and effective vascular occlusion were demonstrated in both swine kidneys and rete mirabile. Contrast from iodinated compounds was temporary, dissipating within hours. The doxorubicin in vitro release profile was linear over 90days. The results demonstrate that GPX is a versatile liquid embolic platform that can be formulated with a wide range of viscosities injectable at clinically practical flow rates, with either transient or permanent contrast, and that can provide prolonged zero-order delivery of doxorubicin to embolized tissues.

Quantification and Validation of an HPLC Method for Low Concentrations of Apigenin-7-O-Glucuronide in Agrimonia pilosa Aqueous Ethanol Extract Topical Cream by Liquid-Liquid Extraction.

In this study, we aimed to develop and validate a pretreatment method for separating and analyzing the small amounts of biomarkers contained in topical cream formulations. Analyzing semisolid formulations that contain low concentrations of active ingredients is difficult. Cream formulations containing an aqueous ethanol extract of 0.1% Agrimonia pilosa is an example. Approximately 0.0013% of apigenin-7-O-glucuronide(A7OG) was contained as a biomarker in the cream. To determine the A7OG content present in the cream formulation, liquid-liquid extraction using dichlormethane was applied. In addition, the volume of the distribution liquid was measured using the peak ratios of the indicator component, A7OG, and an internal standard, baicalin. Subsequently, the A7OG content in the cream formulation was calculated. Using this time-saving method, A7OG can be simply analyzed without additional pretreatment steps, such as evaporation and reconstitution. Moreover, the validation results confirmed that this analytical method met all of the criteria. Consequently, A7OG was successfully isolated from the cream, analyzed, and quantified using the developed method.

Development of multifunctional drug delivery system via hot-melt extrusion paired with fused deposition modeling 3D printing techniques

The model of core–shell structured tablets is gaining increased interest due to its advantages in controlled-release and combinational drug delivery. Through the encapsulation of the drug by the outer shell, this model exhibits huge potential for reduced administration frequency, improved taste-masking, and personalized medication strategy. Although different types of core–shell tablets have been recently developed, most of them focused on the embedding of the solid tablets. Therefore there is still a need to investigate an optimized model in which multiple dosage forms can be loaded. This work uses hot-melt extrusion and fused deposition modeling 3D printing (FDM 3DP) techniques to develop a multifunctional core–shell model for controlled drug delivery. Acetaminophen (APAP) was used as the model drug. Hydroxypropyl cellulose (HPC) and hydroxypropyl methylcellulose (HPMC) was used as the matrix materials. Polyethylene oxide (PEO) and Eudragit RS PO (E RSPO) were used to adjust the printability while the E RSPO was expected to act as an extended-release agent due to its hydrophobicity. Liquid, semi-solid and solid dosage forms could be successfully loaded into the produced shells. The formulations were characterized by scanning electron microscopy, three point-bend tests, differential scanning calorimetry, and dissolution studies. The dissolution results suggested the modified-release character of the designed model. Overall, the designed core–shell model could be successfully produced via hot-melt extrusion paired with FDM 3DP techniques and could be utilized for the delivery of distinct dosage forms which improve the on-demand formulation development for patient-centered medication.

THIOLATED MORINGA EXUDATE GUM AS IMPROVED BIO-MUCOADHESIVE AGENT IN THE FORMULATIONS OF DENTAL PASTE AND GEL

Objective: The objectives of the current study were to synthesize thiolated moringa exudate gum (TMEG) via thiolation of moringa exudate gum (MEG) and to evaluate TMEG as an improved bio-mucoadhesive agent in semi-solid formulations like dental paste and gel. MEG-and TMEG-based mucoadhesive dental pastes of aceclofenac and mucoadhesive gels of metronidazole were prepared and changes in bio-mucoadhesion capability were studied. Methods: In the current study, extracted MEG was modified to synthesize TMEG via thiolation (by utilizing thioglycolic acid in an acidic milieu) to study improvement in bio-mucoadhesive capability. MEG-and TMEG-based mucoadhesive dental pastes of 1% w/w aceclofenac and mucoadhesive gels of 1% w/w metronidazole were prepared with MEG and TMEG (as mucoadhesive excipient) in order to evaluate a comparative view of improvement in bio-mucoadhesion. Results: The yield percentage of TMEG was found to be 44.62% and the thiol group in TMEG was found 4.17 mmol of thiol group/g of MEG. FTIR analysis results indicated the thiolation of MEG in the synthesized TMEG. Both types of semi-solid formulations (mucoadhesive dental pastes of 1% w/w aceclofenac and mucoadhesive gels of 1% w/w metronidazole) prepared using TMEG as mucoadhesive excipient exhibited excellent improved ex vivo bio-mucoadhesion and a sustained pattern of drug-releasing over a prolonged period. Conclusion: The synthesized TMEG can be used as an improved mucoadhesive agent in the designing of bio-mucoadhesive semi-solid formulations for prolonged drug delivery.

Nanoparticle-based chewable gels of praziquantel

Chewable gels present significant advantages over conventional dosage forms, despite their development is not comprehensively assessed. In this sense, six formulations, varying gelatine concentration, dose, and form of incorporation of praziquantel, were developed and characterized. The novelty of this approach focused not only on the development of the formulation itself but also on the incorporation of the drug in a nanoparticulated form. The obtained results for moisture content, water activity, pH, and drug content were within the expected values for this type of formulation. On the other hand, texture and disintegration parameters were influenced by the form of incorporation of praziquantel and the amount of gelatine added. Finally, in vitro dissolution of chewable gels showed significant differences with intermediate products, though the improved dissolution of the nanoparticulated drug was maintained. In conclusion, nanoparticulate drugs can be incorporated into these semisolid formulations and could be successfully applied to other low-aqueous solubility drugs.

Antimicrobial activity of sugar based semisolid polyherbal ayurvedic formulation: Chyawanprash

Antimicrobial activity of sugar based semisolid polyherbal ayurvedic formulation: Chyawanprash