Semisolid Formulations Research Articles

Scale-Up and Postapproval Changes in Orally Inhaled Drug Products: Scientific and Regulatory Considerations.

Approved drug products may be subject to change(s) for a variety of reasons. The changes may include, but are not limited to, increase in batch size, alteration of the drug product constituent(s), improvement in the manufacturing process, and shift in manufacturing sites. The extent of pharmaceutical testing and the regulatory pathway for timely implementation of any change in the approved product and/or process depends upon the nature and extent of change. The U.S. Food and Drug Administration (FDA) has published guidelines that outline its expectations for the Scale-Up and Postapproval Changes (SUPAC) in the solid oral immediate and modified release (MR) products, and semisolid formulations. However, to date, no such guidelines have been issued to address SUPAC in the orally inhaled drug products (OIDPs), and this article represents a seminal contribution in this direction. It is hoped that it will inspire contributions from the relevant multidisciplinary experts from the pharmaceutical industry and the agency in accomplishing formal regulatory guidelines relevant to the OIDP SUPAC. The OIDPs are complex drug-device combination products. Therefore, a conceptualization of SUPAC guidelines for these products warrants consideration of contributions of effect of change(s) in individual components (drug substance, formulation, device) as well as a compound effect that a single or multiple changes may have on product performance, and its safety and efficacy. This article provides a discussion of scientific aspects and regulatory bases relevant to the development of SUPAC for OIDPs, and it attempts to outline considerations that may be applicable in addressing issues related to the OIDP SUPAC in the context of human drugs. The authors' statements should not be viewed as recommendations from any regulatory agency, as the applicable guidelines would be determined on case-by-case evaluation by the relevant authorities.

Enhancing photosynthetic efficiency in Phalaenopsis amabilis through bioreactor innovations

BackgroundMicro-propagation is the primary technique for the mass propagation of greenhouse orchids. However, various factors, including culture media and cultivation systems, influence the scaling-up and efficient commercialization of in vitro techniques. The utilization of liquid cultivation systems and bioreactors are relatively cost-effective and has attracted significant attention for mass production. In this study, we evaluated the effects of eight culture media, in both semi-solid and liquid forms, on the growth of in vitro mini-plantlets of Phalaenopsis orchids. We subsequently assessed the performance of four selected media: half-strength modified Murashige and Skoog (1/2 MMS), modified FAST (MFAST), and two simplified media (SM1 and SM2), across four types of cultivation systems, including semi-solid media in glass jars, liquid media in a permanent immersion system using Erlenmeyer flasks on a shaker (PIS), and a temporary immersion system (TIS) in two forms: FA-Bio bioreactor (TIS-FA-Bio) and RITA® bioreactor (TIS-RITA®).ResultsThe results indicated that the optimal culture medium for orchid growth depends on the cultivation system used. Among the eight evaluated semi-solid and liquid media, the highest plant growth was observed in the SM2 medium, attributed to the presence of additives (banana powder and activated charcoal), two types of sugar (with high carbon content), and small amounts of nickel and ascorbic acid. The high carbon content in the SM2 liquid medium, combined with the temporary immersion explants in a large volume of medium in the TIS-RITA®, resulted in the highest total carbohydrate content and enhanced plant growth. The maximum quantum efficiency of photosystem II (Fv/Fm) and the number of plantlets per liter in SM2 semi-solid medium were higher than those in the 1/2 MMS semi-solid medium (control), leading to a 61.6% reduction in production costs. Furthermore, the number of plantlets per liter in the TIS-FA-Bio containing SM2 (10.8 USD) was higher than in TIS-RITA® with 1/2 MMS (39.3 USD), resulting in a 72.5% decrease in production costs due to a lower volume of medium and the use of inexpensive equipment.ConclusionsWe recommend the use of SM2 in TIS-FA-Bio and TIS-RITA® for economical and efficient mass propagation of Phalaenopsis orchid.

Vesicular phospholipid gels: A new strategy to improve topical antimicrobial dermatotherapy

Therapeutically effective and biocompatible dermal formulations that can ensure localization of a high level of antimicrobial drug at the site of action for an appropriate duration, while at the same time providing intrinsic reepithelization properties, are of particular importance for the treatment of infected and injured skin. The current research aimed to explore the potentials of using vesicular phospholipid gels (VPGs), semisolid formulations consisting of tightly packed liposomes (100–––200 nm), as innovative local depot drug vehicles for advanced topical dermatotherapy. Ciprofloxacin hydrocholoride (CPX) was selected as a model hydrophilic antibacterial drug and was loaded into several VPGs, differing in their composition. Various CPX-loaded VPGs (CPX-VPGs) were evaluated in vitro for the rheological and physicochemical characteristics, drug release profile, stability under in vivo mimicked conditions and during storage, skin permeability, biocompatibility with the epidermal cells, antibacterial efficacy and wound healing assay, to determine the optimal CPX-VPG for topical dermatotherapy. Viscosity and bilayers fluidity of VPGs affected the release of CPX from CPX-VPGs and its skin localization, limiting CPX percutaneous absorption. All CPX-VPGs exhibited even a 2-fold increase in anti-biofilm activity against both Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus (MRSA) clinical isolate compared to the free drug, while showing no toxic effects on human keratinocytes in vitro. Based on the pronounced proliferative effects on keratinocytes, superior in vitro wound healing effect and drug localization on/inside the skin, CPX-VPGs containing chitosan and hydrogenated phospholipid proved to be the most promising for topical dermatotherapy. These findings, along with increased bioadhesiveness and the slow drug release, with CPX concentrations significantly above the minimum biofilm inhibitory concentrations for bacteria typical in infected wounds, would contribute not only to the improvement of the antimicrobial dermatotherapy, but also to reduction of the frequency of the drug administration.

CREMES COSMÉTICOS MANIPULADOS COM VITAMINA C: UMA ANÁLISE QUANTITATIVA

CREMES COSMÉTICOS MANIPULADOS COM VITAMINA C: UMA ANÁLISE QUANTITATIVA

Moisturizing Cream

A cream is a preparation usually for application to the skin. Creams are defines as "a semisolid dosage form containing one or more drug substances dissolved or dispersed in a suitable base

Use of Electrospun Cellulose Acetate/Silica Composites as Multifunctional Ingredients in Eco‐Friendly Semisolid Lubricant Formulations

ABSTRACTCellulose acetate/silica (CA/SIL) nanocomposites are prepared by electrospinning and investigated as multifunctional ingredients in eco‐friendly semisolid lubricant formulations. The structuring ability of these electrospun composites in castor oil and the antifriction and antiwear properties are examined through rheological and tribological experiments. The multifunctionality of CA/SIL composites arises from a balance between the silica content and the formation of nanofiber‐dominated structures. The linear viscoelasticity functions in the oleo‐dispersions increase by several orders of magnitude with both the spinning solution concentration and the CA:SIL ratio. However, the rheological response primarily depends on the morphology of the nanofiber mat obtained, specifically nanofiber diameter and the presence of beads. In contrast, the silica content significantly impacts the tribological performance of the oleo‐dispersions regardless of nanofiber morphology. For similar nanoarchitectures and rheological responses, the friction coefficient is reduced from 0.227 to 0.108 by incorporating silica in a 10:1 CA:SIL ratio, compared with the SIL‐free electrospun CA nanofibers, while wear is completely prevented. Increasing the composite concentration from 5 to 12.5 wt. % enhances wear protection and the gel strength of oleo‐dispersions, for example, the plateau modulus rises from 800 to 42,000 Pa using a composite with a 10:1 CA:SIL ratio.

Semi Solid Dosage from Ointments

Oinment are semisolid formulation commonly used topic administration active pharmacutical ingredient And theraputic uses of oinment in trating various Dermatological and systematic condition oinment are primarily composed base (such as petroleum lanolin or emulsifying wax ) the skin barrier for localized or systemic effect..

Acute oral toxicity study of novel polyherbal formulations by using wistar rats and Swiss albino mice as per OECD 425 TG

BackgroundHydaljss08 is a new semisolid fermented hydroalcoholic polyherbal formulation containing crude drug substances. Immunoboost Tab is a novel polyherbal dosage form that is incorporated isolated, and fractionated phytochemical substances. Acute oral toxicity is a primary safety profile of the novel polyherbal formulations. As a part of our study, we estimated acute toxicity safety profile of novel dosage forms by a Swiss albino mice and Wistar rats. AimAccording to the OECD 425 test guideline., the study aims to estimate acute toxicity tests of the “Hydaljss08, and Immunoboost Tab” dosage forms in rats and mice to assess the safety profile. Mice and rats are normally used in safety studies because of their susceptibility to toxic challenges, tumor induction, and carcinogenicity. Material and Methods1 % CMC, Hydaljss08, Immunoboost-Tab polyherbal formulations, female rats, and albino mice. Animals were divided into the control groups, and treated groups with test dosage forms. At the end of the study, animals were euthanized by using the CO2 asphyxiation technique and subjected to gross pathological examinations. ResultsAccording to the assessment of the experimental data, the single-dose acute toxicity study of Hydaljss08 and Immunoboost-Tab formulations in mice and rats was fine. No signs of toxicity were observed in the animals treated at (2000 mg/kg.b. wt, Po), and revealed dullness, causing lethargy, and piloerections, which only persisted on the 1st day. At the end of the study, mild congestion in the liver, and lungs was observed in animals, treated with “Hydaljss08 formulation” compared to the vehicle control groups. ConclusionsThe estimated LD50 of Hydaljss08, and Immunoboost-Tab polyherbal formulations in rats and mice by oral route was found >2000 mg/kg, b.wt.

Synthetic membrane selection for in vitro release testing (IVRT): A case study of topical mometasone furoate semi-solid dosage forms

In vitro release testing (IVRT) is extensively used to develop the formulation of topical semi-solid products, to evaluate the quality and consistency of the product after scale-up and post-approval changes, and more recently to aid the evaluation of topical generic products’ equivalency. The selection of synthetic membrane is one of the most critical parameters of the method development part of IVRT. It is well known that the membrane features namely its polymer matrices, porosity, pore size, thickness can have a substantial effect on the IVRT data. However, there is no detailed information available in the literature regarding the membrane selection for different types of topical dosage forms. Therefore, we aimed to investigate whether difference topical semi-solid dosage forms of the same drug molecule would cause to variation in the membrane selection. Within this framework, rheological behaviour of commercially available three different types of topical semi-solid dosage forms (ointment, cream, and lotion) of mometasone furoate (0.1%) were primarily characterized. Then, the membrane inertness test was conducted using a series of synthetic hydrophilic membranes (regenerated cellulose, cellulose acetate, cellulose nitrate, mixed cellulose ester membranes) and hydrophobic membranes (polyether sulfone, polypropylene, polytetrafluoroethylene membranes) after identifying of an appropriate receptor medium that ensures sink condition for mometasone furoate. Lastly, IVRT studies from the topical semi-solid products were performed utilizing Franz-type diffusion cells. The membrane inertness and in vitro release data demonstrated that the cellulose acetate membrane showed superior diffusion properties in general while the other synthetic membranes exhibited varying outcomes for different semi-solid dosage forms of mometasone furoate. Overall, the results indicated that the release rate and the cumulative drug released amount of drug after 6 h through the different synthetic membranes might vary depending on the semi-solid dosage form. In order to select the synthetic membrane for IVRT, it should also be considered potential interactions between the polymer matrices and the chemical structure of drug molecule as well as formulation components prior to conducting membrane inertness test and IVRT studies.

The effect of Amazonian andiroba oil on antioxidant activity, mechanical, rheological and skin permeation properties of environmentally responsive emulgels

Emulgels are semi-solid systems that can improve the bioavailability of bioactive agents by combining the properties of gels and emulsions in a stable way. The use of bioadhesive systems by combining different polymers can prolong the release of various bioactive agents, such as the oil of Carapa guianensis (andiroba oil; AO), which has been of interest to researchers for years due to its antioxidant properties, antitumor, antibacterial and anti-inflammatory activity. Therefore, the aim of the present work was to evaluate the influence of different amounts of AO on the physicochemical properties of thermoresponsive bioadhesive emulgels composed of Carbopol 974 P® and poloxamer 407. The mechanical, rheological, bioadhesive, skin permeation and antioxidant activity characteristics were analyzed. AO and emulgel systems showed a potential antioxidant effect via different mechanisms. The formulations also displayed important results in terms of textural mechanical, bioadhesiveness, rheological and skin retention characteristics. However, F1 showed more promising results than F2, with differences mainly in softness, bioadhesion and rheology. These results ensure favorable properties for potential use as a topical semi-solid formulation and for therapeutic applications. However, additional studies are necessary to explore their in vitro biological and in vivo performance.

Development And Validation of In-Vitro Release Test (IVRT) Method for Topical Complex Generic - Ganciclovir Ophthalmic Gel

Background: The in-vitro release test (IVRT) is a tool to measure the amount and the release rate of active pharmaceutical compounds released from topical semisolid dosage forms. The IVRT provides significant information for product performance assessment and evaluation. It is also used to assess the bioequivalence study (biowaivers) for topical semisolid products. Objective: The study aims to develop and validate the IVRT method for qualitative and quantitative estimation of ganciclovir topical products and to demonstrate the similarity between the marketed reference product and the in-house test product of ganciclovir ophthalmic gel. Method: The method was developed using a vertical diffusion cell with a synthetic cellulose membrane, simulated tear fluid as the receiver media, and UV detection. The IVRT study was performed at 100rpm and 32oC for 6hr. The marketed formulation containing 0.15%w/w ganciclovir was used as a reference. Result: The in-house test product of ganciclovir met all characterization criteria. The analytical method was optimized and validated with a concentration range of 2-14μg/ml and a regression coefficient of 0.9997 as per the ICH guideline. The developed IVRT method was simple, economical, linear, robust, reproducible, sensitive, specific, and selective to evaluate the drug release from the formulation. The %recovery at 6hr was found to be 84.43% and 78.68% for reference and test product of ganciclovir ophthalmic gel with correlation coefficient R2 0.9947 and 0.9921, respectively, this value justified the biowaivers between the reference and test formulation. Conclusion: This method can be utilized to check topical semisolid product quality, product performance, and product uniformity. Additionally, it can also be used to waive the requirement for bioequivalency studies for ganciclovir ophthalmic gel.

Impact of salt strength on in vitro propagation and rebaudioside A content in Stevia rebaudiana under semi-solid and liquid MS media.

Stevia rebaudiana (Bertoni), commonly known as stevia, is a sought-after natural sweetener, but its conventional propagation methods are slow and inefficient. This study aims to enhance the in vitro culture for stevia by investigating the impact of different Murashige and Skoog (MS) medium salt strengths and plant growth hormones on growth and rebaudioside A content. Apical bud-containing shoot segments were used as explants and cultured on various semi-solid and liquid MS media formulations, incorporating cytokinins (BAP and Kin), auxins (NAA and IAA), and different MS major salt concentrations (MS full, ½ MS, and ¼ MS). Assessments of shoot growth parameters, root formation, and HPLC analysis for rebaudioside A content were conducted. The optimal conditions for in vitro growth was found to be in the ¼ MS + Kin 3mg/L + NAA 0.1mg/L (semi-solid) medium, resulting in significantly improved shoot growth and enhanced 30.04% rebaudioside A content. Genetic fidelity of regenerated plants was confirmed using RAPD and ISSR markers. These findings offer valuable insights for optimizing in vitro propagation of stevia and potentially enhancing rebaudioside A content.

Retinol and Oligopeptide-Loaded Lipid Nanocarriers as Effective Raw Material in Anti-Acne and Anti-Aging Therapies

The use of lipid nanocarriers as components of cosmetic formulations may provide an opportunity to fully exploit the beneficial properties of pentapeptide-18 and retinol while reducing the undesirable effects that occur during retinoid therapy. This study aimed to evaluate the effectiveness of semi-solid formulations enriched with retinol and oligopeptide-loaded lipid nanocarriers. Solid lipid nanoparticles were produced using a high-shear homogenization method. The work included physicochemical characterization of the cosmetic products, and evaluation of their stability as well as their efficacy. The resulting semi-solid preparations were determined to be stable regardless of their storage temperature. No effect of the presence of lipid nanoparticles on the shelf-life stability of the cosmetic products was observed. A temperature of 25 °C was considered the recommended storage temperature for the tested semi-solid formulations. Beneficial effects of the cosmetic products were proven (in vivo study on volunteers), i.e., a significant reduction in the level of sebum secretion (anti-acne therapy) and a decrease in the number of facial wrinkles (anti-aging therapy). In addition, the protective properties of the lipid nanoparticles themselves against the skin were confirmed, reducing the irritating effect of retinol that is usually the case with classic retinoid therapies.

Study of the Effect of Phosvitin as a Potential Carrier on the Permeation Process of Somatotropin (STH) and Corticotropin (ACTH) from Biodegradable Polymers Used as Vehicles for STH and ACTH in Semi-Solid Formulations for Skin Application.

Phosvitin shows chelating abilities, an affinity for ACTH (corticotropin), growth factors, antioxidant properties, and acidic nature. An attempt was made to use this protein in hydrogels as a transporter of other protein substances: somatotropin (STH) and (ACTH). The aim of the study was to evaluate the effect of phosvitin on the permeation of ACTH and STH from semi-solid forms of the drug applied to the skin. Four hydrogel substrates were prepared using natural polymers: sodium alginate, methylcellulose, and starch. Based on the evaluation of physicochemical parameters, the hydrogel with the most favorable properties was selected and loaded with the active substances STH and ACTH, followed by the addition of phosvitin. A study of the permeation of STH and ACTH through the artificial cellulose membrane and through porcine skin was carried out without and with the addition of phosvitin. The effect of protein substances on rheological and textural parameters was studied. The evaluation of physicochemical parameters showed a favorable effect of STH and Phosvitin on the stability of the hydrogel with 4% methylcellulose and no effect of ACTH. All prepared formulations showed a reaction close to the natural pH of human skin. In the porcine skin permeation study, the addition of Phosvitin to the hydrogel with STH caused a slight increase in the amount of STH permeated and an increase in the time for STH to permeate porcine skin by 30 min. Phosvitin caused an increase in the amount of ACTH permeated through porcine skin almost twofold. Phosvitin may prove to be a promising permeation promoter for model protein-peptide substances when applied to the skin surface.

Acai Oil-Based Organogel Containing Hyaluronic Acid for Topical Cosmetic: In Vitro and Ex Vivo Assessment.

Organogels are semi-solid pharmaceutical forms whose dispersing phase is an organic liquid, for example, an oil, such as acai oil, immobilized by a three-dimensional network formed by the gelling agent. Organogels are being highlighted as innovative release systems for cosmetic active ingredients such as hyaluronic acid for topical applications. Acai oil was evaluated for its physicochemical parameters, fatty acid composition, lipid quality index, spectroscopic pattern (Attenuated total reflectance Fourier Transform Infrared Spectroscopy), thermal behavior, total phenolic, total flavonoids, and total carotenoids and β-carotene content. The effectiveness of the organogel incorporated with hyaluronic acid (OG + HA) was evaluated through ex vivo permeation and skin retention tests, in vitro tests by Attenuated total reflectance Fourier Transform Infrared Spectroscopy and Differential Scanning Calorimetry. The physicochemical analyses highlighted that the acai oil exhibited quality standards in agreement with the regulatory bodies. Acai oil also showed high antioxidant capacity, which was correlated with the identified bioactive compounds. The cytotoxicity tests demonstrated that the formulation OG + HA does not release toxic substances into the biological environment that could impede cell growth, adhesion, and efficacy. In vitro and ex vivo analyses demonstrated that after 6 h of application, OG + HA presented a high level of hydration, thermal protection and release of HA. Thus, it can be concluded that the OG + HA formulation has the potential for physical-chemical applications, antioxidant quality, and potentially promising efficacy for application in the cosmetic areas.

Dual Chemotherapeutic Loading in Oxalate Transferrin-Conjugated Polymersomes Incorporated into Chitosan Hydrogels for Site-Specific Targeting of Melanoma Cells.

In this work, we developed a smart drug delivery system composed of poly (ethylene glycol)-block-poly (ε-caprolactone) (PEG-PCL)-based polymersomes (Ps) loaded with doxorubicin (DOX) and vemurafenib (VEM). To enhance targeted delivery to malignant melanoma cells, these drug-loaded nanovesicles were conjugated to the oxalate transferrin variant (oxalate Tf) and incorporated into three-dimensional chitosan hydrogels. This innovative approach represents the first application of oxalate Tf for the precision delivery of drug-loaded polymersomes within a semi-solid dosage form based on chitosan hydrogels. These resulting semi-solids exhibited a sustained release profile for both encapsulated drugs. To evaluate their potency, we compared the cytotoxicity of native Tf-Ps with oxalate Tf-Ps. Notably, the oxalate Tf-Ps demonstrated a 3-fold decrease in cell viability against melanoma cells compared to normal cells and were 1.6-fold more potent than native Tf-Ps, indicating the greater potency of this nanoformulation. These findings suggest that dual-drug delivery using an oxalate-Tf-targeting ligand significantly enhances the drug delivery efficiency of Tf-conjugated nanovesicles and offers a promising strategy to overcome the challenge of multidrug resistance in melanoma therapy.

Physical Test of Avocado Leaf Extract Cream Formula

Avocado (Perseaamericana Mill) is a plant that grows widely in subtropical and tropical areas, one of which is Indonesia. The leaves of the avocado plant, which we can use as traditional medicine, are reported to be anti-bacterial and can inhibit the growth of several bacteria, including Staphylococcus aurus. The active substances contained in avocado leaves are flavonoids, quercetin and tannin which are useful as anti-bacterials and as a source of natural antioxidants. This study aims to determine the results of the physical test of the avocado leaf extract cream formula. This type of research is quantitative with a descriptive research design. In testing the cream, an organoleptic test, homogeneity test, pH test, spreadability test, absorption test and adhesion test were carried out. The results obtained in the organoleptic test were seen from the yellowish brown color, the semi-solid dosage form, and the distinctive creamy smell of avocado leaves, the homogeneity test of the cream did not occur in phase separation, namely the water phase and the oil phase, the pH test of the cream had a pH of 7, the power test Spread the cream with a diameter of 6.1 cm, the cream's absorption test can absorb water optimally, and the cream's adhesion test obtains an adhesion time of 1.48 seconds. The physical test of the avocado leaf extract cream formula meets the requirements.

Microbiological and Analytical Evaluation of Semi-Solid Formulations of Doxycycline Hyclate under Accelerated Stability Conditions

الدوكسيسكلين هايكلات هو مضاد حيوي واسع الطيف ينتمي لعائلة التتراسيكلينات، يستخدم بشكل واسع في معالجة العديد من الأمراض الالتهابيًة، ويعتبر الخط العلاجي الأوًل في تدبير الحالات المتوسطة إلى الشديدة من حب الشًباب. تم في هذا البحث صياغة أربع صيغ نصف صلبة للدوكسيسيكلين (F2,F1 كصيغ هلاميًة، F3,F4 كصيغ مرهميًة)، ثم عُرّضت الصيغ السابقة إلى شروط ثبات مسرًعة في حاضنات الثبات لمدة ثلاثة أشهر. تم تقييم الصيغ المحضرة باستخدام طرق ميكروبيولوجيًة وتحليلية وذلك خلال شهر وثلاثة أشهر. استخدمت طريقة الانتشار على الآغار لتقييم الفعاليًة المضادة للجراثيم وذلك على نوعين من الجراثيم، العنقوديات المذهًبة والزائفة الزنجاريًة. بينما استخدم HPLC كطريقة تحليل كمية وكيفية لمقايسة الصيغ. أجريت مقارنة بين نتائج المقايسة الميكروبيولوجيًة والمقايسة التحليلية لتقييم الفعاليًة. أظهرت النتائج أن الصيغ المرهميّة F3,F4 أكثر ثباتاً من الصيغ الهلاميّة F1,F2، حيث بلغت النسبة المئوية للدوكسيسيكلين % 93و%91 للصيغة F3,F4 على التوالي وذلك عند الحفظ بدرجة حرارة الغرفة بعد شهر واحد. بينما بلغت النسبة%90 و65% للصيغ الهلاميّةF2,F1 عند الحفظ في نفس الشروط السابقة. أظهرت نتائج قياس الفعاليًة المضادة للجراثيم أن الصيغة المرهميًة F4 امتلكت أكبر قطر تثبيط جرثومي ويقدر بحوالي 31 ملم للعنقوديات المذهبة و26 ملم لـلزوائف الزنجارية وذلك بعد حفظ الصيغة لمدة ثلاثة أشهر عند درجة الحرارة 25ºم. وبالتالي حافظت الصيغ على فعاليتها على الرغم من التخرّب الكيميائي البنيوي للحاصل للدوكسيسيكلين. تعود هذه الفعالية إلى حقيقة أن نواتج التخرب لا تزال محافظة على الموقع البنيوي الفعًال والمسؤول عن إعطاء الفعاليًة المضادة للجراثيم.

Characterization of Structure-Surface Correlations in Ointments Using Surface Tensiometry within the Concept of an Integrated Analytical Approach.

In recent years, integrated data analysis has proven to be a valuable method for investigating complex systems, whether artificial or natural. The integrated analytical approach allows the simultaneous integration of data acquired from different analytical techniques employed for the same sample at the same time, leading to an expansion of the amount of information available. Surface tensiometry is a technique that was recently introduced in the Integrated Analytical Approach for investigating pharmaceutical dosage forms for topical application. Therefore, studies of rheological characterization, release, and skin permeation can be integrated with surface tensiometry measurements to develop chemical and rheological-surface correlation models, providing a new method for the quality control and process control of semisolid preparations. In this context, the aim of this research is to validate the utility of surface tensiometry measurements in the Integrated Analytical Approach and utilize these data to gain insights into the structure-surface correlation. The preparations chosen for this study were a PEG-gel, a lipogel, and an O/W cream containing carnitine as a model drug. The formulations were characterized using rheological measurements and evaluated for their carnitine release performance. Furthermore, surface tensiometry measurements were performed to rapidly and noninvasively assess the influence of carnitine on the surface properties of the semisolid preparations investigated. Our work demonstrated a close correlation between surface energy and structural data, showing the importance of surface tensiometry contribution in the noninvasive and rapid evaluation of the presence of carnitine in semisolid formulations.

Bioadhesive gel containing 5 % acyclovir for the treatment of herpes labialis: Preclinical development

Acyclovir is widely indicated for the treatment of herpes labialis, an infection typically caused by herpes simplex virus 1 (HSV-1). The standard treatment is based on the use of this antiviral in conventional topical semi-solid formulations (ointments, creams or gels), which have limitations such as low skin adherence and poor patient compliance. On the other hand, therapeutic bioadhesive gels (TBG) are semi-solid formulations that form a thin and transparent polymeric film in situ, displaying superior cosmetic attributes than conventional semi-solid forms and offering improved skin maintenance and patient compliance. In this study, a TBG containing 5 % of acyclovir was developed and characterized in terms of assay, impurities, appearance, pH, viscosity, particle size and morphology and microbiology count, complying with specifications. Stability studies showed that acyclovir-TBG was stable for at least 3 years under the experimental conditions carried out according to the International Council for Harmonisation (ICH) guidelines. Moreover, its cosmetic attractiveness and film-forming ability were considered positive and the in vitro penetration studies revealed a 23.8-fold increase in acyclovir retained percentage in the skin compared to the reference product Zovirax® (11.9 vs 0.5 % after 24 h, respectively). Finally, in vivo skin and ocular irritation studies as well as dermal tolerance studies did not show any negative sign in the macroscopic and microscopic examination. Thus, the proposed formulation could be a good and safe alternative for the topical treatment of lesions caused by HSV-1.