The continuous emergence of new pathogens and the evolution of microbial drug resistance make it absolutely necessary to develop innovative, effective vaccination strategies. Use of nasal vaccination can increase convenience, safety, cause both local and systemic immune reactions. Intranasal administration nevertheless has a number of shortcomings that can be overcome by using the latest achievements of pharmaceutical science. One of the aspects of such solution may be the use of systems for the production of intranasal vaccines in situ polymer compositions that provide a directed sol-gel transition controlled by the physiological conditions of the nasal cavity. At the same time, the gelation of the administered dose in contact with the nasal mucosa involves prolonged exposure of the drug at the injection site, greater mucoadhesion, counteraction to mucociliary clearance, modified and more complete release. A number of both foreign and domestic manufacturers produces polymers such as chitosan, gums, polyoxyethylene and polyoxypropylene block copolymers (poloxamers, proxanols), carbomers. For effective pharmaceutical development of new intranasal IBD delivery systems corresponding to the QbD concept, not only the knowledge of the range of excipients is necessary, but also simple, accessible, and reproducible methods for determining indicators that define the critical parameters of such delivery systems. In accordance with the conducted scientific search, the main indicators of standardization of in situ intranasal systems were identified: temperature and time of gel formation, gel strength, rheological characteristics, mucoadhesion, release, nasal mucociliary clearance time.
Introduction. Effective delivery of ophthalmic drugs is challenging. The eye has a number of protective systems and physiological barriers, which is why ophthalmic dosage forms have a low bioavailability, usually not exceeding 5 %. Topical drug administration is relatively easy to use and is most commonly prescribed by physicians for the treatment of ophthalmic diseases, especially the anterior segment of the eye. However, when using traditional delivery systems, a number of problems arise: patients' violation of the drug administration technique, and, as a consequence, a decrease in treatment compliance, restriction of drug delivery to the target eye tissues due to low epithelial permeability and rapid clearance after drug administration. Maintaining a constant therapeutic drug level is another challenge that traditional delivery systems often fail to cope with.Text. The article discusses the types of ophthalmic delivery systems. Traditional ones are represented by such dosage forms as eye drops, ointments, gels. Modern ophthalmic dosage forms are represented by: eye films, contact lenses and eye implants. The characteristics, advantages and disadvantages of each type of delivery systems and their promising directions of development, as well as modern developments in this area are given.Conclusion. Currently, most of the scientific research on the development of ophthalmic delivery systems is devoted to obtaining dosage forms capable of maintaining a constant concentration of the drug in the target tissue, providing the transport of active ingredients to them. This is achieved by using modern advances in nanotechnology and polymer chemistry. Receive liquid and soft dosage forms with micro-, nano- and micro-nano-carriers. Polymeric delivery systems such as films, lenses and implants are being actively developed and studied. The development of modern technological approaches opens up new possibilities for the treatment of a wide range of ophthalmic diseases by reducing the side effects often induced by the intrinsic toxicity of molecules, reducing the frequency of the administered dose and maintaining the pharmacological profile of the drug. Thus, the use of modern ophthalmic delivery systems can significantly limit the use of invasive treatments.
BACKGROUND: In recent years, mucoadhesive dosage forms due to their advantages have attracted the interest of researchers and developers. Polymeric excipients are included into the drug composition to give adhesion to the mucous membrane. AIM: The aim of this research was to select a specific brand of pharmaceutical quality polymer that is promising for inclusion in the drug formulation. METHODS: The article presents the results of studying the mucoadhesive properties of polymers on two models using mucin: By measuring the amount of adhesion and by the evaluation the sample movement speed. RESULTS: According to the combination of two indicators, the highest mucoadhesive properties were shown by the brands of hydroxypropylmethylcellulose and xanthan gum. In addition, it was noted that hydroxyethylcellulose (HEC), sodium alginate, and hydroxypropylmethylcellulose (HPMC) also have good mucoadhesive properties. Polyethylene glycols proved to have the weakest mucoadhesive properties. The negative relationship between the average molecular weight and the sample movement speed of the HEC and HPMC was established. Obtained data showed no direct influence of the polymer average molecular weight on the amount of adhesion. It was also noted that there is no strong correlation between the amount of adhesion and the sample movement speed of the experimental samples. CONCLUSION: Based on the results of the study, it was suggested that the complex influences of the physical and chemical properties of the polymer on its mucoadhesive properties.
Introduction. Dental gel is one of the modern dosage forms with optimal biopharmaceutical properties for the treatment and prevention of oral diseases An isoquinoline alkaloid berberine is the promising active substance with antibacterial and anti-inflammatory effect, capable of forming stable dispersed systems with gel-forming components. It is noteworthy that, despite the pronounced antimicrobial activity of the alkaloid berberine, there is currently no dental dosage form with this component on the pharmaceutical market, and therefore research in this direction is of great interest.Aim. Selection of the optimal technology for obtaining dental gel with berberine for the treatment of oral diseases.Materials and methods. Berberine bisulfate (manufactured by CJSC «Vifitech», Obolensk, Moscow region, RF), poloxamers P407 and P338 (EP, USP/N; BASF, Germany), propylene glycol (USP; BASF, Germany), sodium chloride (Sigma-Aldrich, Germany, Cat. No. S9888), mucin type II from a pig stomach (Sigma-Aldrich, Germany, Cat. No. M2378). In the development of the composition and technology for the preparation of gels, a magnetic stirrer with a temperature control function (C-MAG HS 7 from IKA, Germany) was used. Gels were prepared by the «hot method» and «cold method».Results and discussion. The production of the gel by the «hot method» provided a uniform dosage form. The obtained pH value is within the range of optimal diapason. Measurement of the specific peel force of the model gel sample showed pronounced mucoadhesive properties, which indicates that there is no need to adjust this parameter by introducing additional components into the formulation. The spectroscopic method is applicable for the analysis of berberine gel. It has been found that a significant dilution of the reference substance sample is required to develop an identification procedure.Conclusion. The production of a sample of the dosage form by the «hot method» is optimal, which is probably due to the effect of solubilization and better distribution of the active substance in the base.
Aim to consider the potential prospects of using Poly(l-lactide-co-glycolide) (PLGA) and shellac to obtain phase-dependent in situ implants. Material and methods. The study required two stages: stage I was the evaluation of NMP-polymer compositions, and stage II was the evaluation of NMP-polymer-PEG compositions. We used PLGA with various ratios of lactide and glycolide units (75:25, 50:50), dewaxed bleached shellac, N-methylpyrrolidone (NMP) as a solvent, and PEG-1500 at a concentration of 5% (wt/vol) as a co-solvent. The experimental formulations contained matrix formers at a concentration of 33%. The formulations were screened for polymer solubility in NMP, homogeneity and permeability through the needle of the resulting polymer-NMP system, the implant formation rate during the liquid-liquid extraction in a phosphate buffer solution (pH=6.8), and the implant morphology. The rate of implant formation and the diffusion of the dye from the delivery systems were also studied using the in vitro agar gingiva model, previously developed in the laboratory of the A.P. Nelyubin Institute of Pharmacy. Results. The first stage of the study showed that the NMP-PLGA system (75:25) formed a solid implant in 1 hour, and the NMP-shellac system in 2 hours. The formulations were positively assessed according to the presented criteria, despite the very different diffusion volumes 1414 l for NMP-shellac and 1065 l for NMP-PLGA (75:25) which indicates the possibility of their use without the introduction of additional excipients. The NMP-PLGA system (50:50) had not completely precipitated after the critical time (3 hours) and was considered as requiring an adjustment due to the insufficient implant formation rate. In the stage II, a less intense diffusion of the dye from the implants into agar was observed. For example, for NMP-PLGA(50:50) 641 l, and for NMP-PLGA(50:50)-PEG 25 l. At the same time, there was the positive dynamics in the time of their precipitation both in phosphate buffer medium (instantaneous precipitation without the need for shaking) and in the in vitro agar gingiva model after 3 hours, the composition of NMP-PLGA (50:50)-PEG, in contrast to NMP-PLGA (50:50), had formed a semi-solid implant. Conclusion. In the course of the experiments, the compositions of NMP-shellac and NMP-PLGA (75:25) were selected as the most promising for further development of a phase-sensitive in situ dental implant. The addition of PEG was found to be rational in terms of increasing the rate of implant precipitation and reducing the initial diffusion of the solvent.
Abstract. The potential of spray film-forming systems for prevention and therapy of peristomal complications is highly significant. The advantages of the dosage form include creation of protective skin barrier, prolonged release of active substances of anti-inflammatory, antiseptic, regenerative spectrum of action, etc. Polymeric compositions can delay and partially prevent the aggressive media impact released by stomas via osmotic action and neutralize the allergic potential of adhesives for attachment of stoma and pouching system. A flexible and thin film can be created via controlled spraying that follows the skin texture, interrupting the irritation "vicious circle". The pH of the composition will reduce the pH of the irritated skin and related microbial contamination. Creation of such form will significantly improve stoma patients’ life quality, prevent some peristomal complications and facilitate skin care surrounding stoma, especially in difficult postoperative periods. The aim was to establish the potential of spray film-forming systems and the prospects of drug development in such a new dosage form to prevent peristomal complications as maceration, allergic dermatitis, and infection complications of mechanical injuries of bacterial and fungal nature, to determine the main properties required from the resulting film, as well as relevant active substances spectrum. In addition, two types of medications were suggested to help patients with self-diagnosis of stoma discharge on the surrounding skin and partially prevent irritation until the problem is detected.
Abstract. The spread of ophthalmic infectious diseases around the world and uniformity of the market of dosage forms for their therapy generate an incentive for scientists to develop innovative drug forms, to create improved therapy for such diseases as uevitis, conjunctivitis, keratitis and blepharitis. There are two types of eye dosage forms on the market of the Russian Federation - drops and ointments, which have a short shelf life after the first application, a high risk of microbial infection and infection of a "healthy" eye. Based on these facts, the study aims to develop a solid extended dosed biodegradable ocular insert for use in ophthalmotherapy. This article is devoted to the peculiarities of influence of film forming agents of different nature, plasticizer and solubilizing agent (poloxamer) and their ratio on the biopharmaceutical properties of the polymeric base of ocular insert. Polymers of both natural and semi-synthetic nature (hydroxyethylcellulose, sodium alginate, xanthan and gellan gum) were used to create the polymeric basis. Placebo inserts were formed at room temperature in open space for three days. The test of the samples was carried out according to the parameters of description, elasticity, dissolution time, humidity, which include in the State Pharmacopeia XIV, and mucohedhesion, that is an important parameter for locally administering on mucosa, although it is not regulated in official documents. The series of experiments showed the optimum concentrations and ratios of the auxiliary substances used, namely 0.5% to 2.5% for film type manufacturers, 2% for plasticizers and 0.5% for poloxamers, respectively. The formulations that showed the best performance when evaluating the parameters were - sodium alginate 2.5%, glycerin 2%, poloxamer 0.5%, water purified up to 40.0; xanthan gum 0.4%, glycerin 2%, poloxamer 0.5%, water purified up to 40.0.have a wide variation in different age categories, which requires further study. on additional samples of children in the region.
Introduction. Infectious otitis externa and middle ear can cause hearing loss, which significantly reduces the quality of life of patients. The main causative agents of acute bacterial otitis media are Pseudomonas aeruginosa and Staphylococcus aureus. This article is devoted to the development and study of a novel dosage form for treatment of infectious diseases of the external ear containing bacteriophages that lyse bacterial strains of Pseudomonas aeruginosa. Ear drops were considered as a promising dosage form for instillation into the ear canal.Aim. The aim of the work is to develop a dosage form of Pseudomonas aeruginosa bacteriophages for the local treatment of infectious otitis media.Materials and Methods. The active substances of the developed drug are bacteriophages that lyse bacterial strains of Pseudomonas aeruginosa: PA5 and PA10, which were obtained by growing on a solid growth medium in mattress flasks with subsequent sterilizing filtration through a membrane filter (0,22 µm) and elimination of endotoxins on a chromatographic column. To obtain experimental compositions, excipients that do not cause a drop in the titer of bacteriophages were used – purified water as the solvent, viscosity modifiers: glycerol (CHIMMED, Russia) and a mix of macrogol 6 and glyceryl caprilocaprate brand Softigen 767 (Cremer, Germany), antioxidant Ethylenediaminetetraacetic acid (EDTA), preservatives nipagin and nipazole. The obtained samples were standardized according to pharmacopoeial indicators, recommended for the dosage form "drops" – density, pH, viscosity. For all experimental compositions, the stability of the titer of bacteriophages was studied by the Gratia method for 6 months. The local irritation and systemic effects were also studied on five chinchilla male rabbits.Results and discussion. As a result of the conducted research, four experimental compositions of ear drops with a cocktail of bacteriophages PA5 and PA10 were obtained. The optimal technological characteristics were observed in the composition containing glycerol as a viscosity modifier at a concentration of 10,0 %. For optimal composition, the stability of the bacteriophages cocktail titer, local irritating and systemic effects were analyzed. The study revealed stability of the bacteriophages PA5 and PA10 titers in the composition of dosage form, and absence of local irritating and systemic effects of ear drops.Conclusion. The dosage form can be recommended for preclinical studies.
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