Search

Solanum surattense Burm. f. is a significant member of the Solanaceae family, and the Solanum genus is renowned for its traditional medicinal uses and bioactive potential. This systematic review adheres to PRISMA methodology, analyzing scientific publications between 1753 and 2023 from B-on, Google Scholar, PubMed, Science Direct, and Web of Science, aiming to provide comprehensive and updated information on the distribution, ethnomedicinal uses, chemical constituents, and pharmacological activities of S. surattense, highlighting its potential as a source of herbal drugs. Ethnomedicinally, this species is important to treat skin diseases, piles complications, and toothache. The fruit was found to be the most used part of this plant (25%), together with the whole plant (22%) used to treat different ailments, and its decoction was found to be the most preferable mode of herbal drug preparation. A total of 338 metabolites of various chemical classes were isolated from S. surattense, including 137 (40.53%) terpenoids, 56 (16.56%) phenol derivatives, and 52 (15.38%) lipids. Mixtures of different parts of this plant in water–ethanol have shown in vitro and/or in vivo antioxidant, anti-inflammatory, antimicrobial, anti-tumoral, hepatoprotective, and larvicidal activities. Among the metabolites, 51 were identified and biologically tested, presenting antioxidant, anti-inflammatory, and antitumoral as the most reported activities. Clinical trials in humans made with the whole plant extract showed its efficacy as an anti-asthmatic agent. Mostly steroidal alkaloids and triterpenoids, such as solamargine, solanidine, solasodine, solasonine, tomatidine, xanthosaponin A–B, dioscin, lupeol, and stigmasterol are biologically the most active metabolites with high potency that reflects the new and high potential of this species as a novel source of herbal medicines. More experimental studies and a deeper understanding of this plant must be conducted to ensure its use as a source of raw materials for pharmaceutical use.

Introdução: A qualidade dos medicamentos tem sido inaceitável em muitas regiões do mundo, especificamente em países subdesenvolvidos, devido à escassez ou ausência total de laboratórios de controlo de qualidade de medicamentos (Devall, 2013). De facto, medicamentos falsificados ou de baixa qualidade constituem uma séria preocupação para a saúde pública, particularmente em países onde os sistemas de vigilância são fracos e ineficientes. Países como Índia, China, Vietname, Indonésia, Paquistão ou Filipinas têm sido identificados como os principais produtores de medicamentos falsificados; ao passo que, China (Hong Kong), Emirados Árabes Unidos, Egipto, Camarões e Turquia parecem ser os principais pontos de trânsito destes produtos farmacêuticos falsificados enviados para o resto do mundo (OCDE, 2020). Objetivo: Avaliação de vários métodos empregados para analisar a qualidade de Medicamentos. Material e Métodos: Foram coletados comprimidos com fármacos anti- inflamatórios não esteroides (AINEs) e antimaláricos, tais como, Zibufeno (Ibuprofeno 400mg), Diclomex 100 (Diclofenac sódico), Amidol® (paracetamol 500 mg), Quini PLUS®-500 (Quinino Sulfato) e Quini PLUS®-300 (Quinino Sulfato), obtidos de vendedores no mercado da Retranca, localizado no município de Cacuaco, província de Luanda, Angola e analisados por Calorimetria Diferencial de Varrimento (DSC), Espectroscopia de Infravermelho com Transformada de Fourier (FTIR) e Difração de Raios-X em Pó (XRPD) (Vueba et al., 2013). Resultados: Confirmou-se a presença da substância ativa como Zibufen e Amidol por DSC, FTIR e XRPD nos comprimidos; enquanto o Diclomex 100 não permitiu a identificação do diclofenac sódico no comprimido. Além disso, o sulfato de quinino no Quini Plus 500 mg e 300 mg só foi identificado por FTIR e XRPD. A análise das substâncias estudadas mostrou que durante a análise térmica podem ocorrer fenómenos como desidratação e (ou) fusão, e transformação cristalina. Conclusões: O estudo demonstrou a aplicação bem-sucedida dos métodos analíticos para avaliar a qualidade dos medicamentos. Os resultados desta investigação vão permitir à monitorização contínua da qualidade dos medicamentos comercializados para garantir a segurança e eficácia destes produtos no tratamento de muitas doenças em Angola.

The successful integration of hot-melt extrusion (HME) and fused deposition modelling (FDM) depends on a better understanding of the impact of environmental conditions on the printability of formulations, since they significantly affect the properties of the raw materials, whose control is crucial to enable three-dimensional printing (3DP). Hence, the objective of this work was to investigate the correlation between the environmental settings and the properties of paroxetine (PRX)-loaded filaments, previously produced by HME, which affect printability by FDM. The influence of different drying methods of the physical mixtures (PMs) and HME-filaments (FILs) on the quality and printability of these products was also assessed. The printability of FILs was evaluated in terms of the water content, and the mechanical and thermal properties of the products. Stability studies and physicochemical, thermal, and in vitro dissolution tests were carried out on the 3D-printed tablets. Stability studies demonstrated the high ductility of the PRX loaded FILs, especially under high humidity conditions. Under low humidity storage conditions (11% RH), the FILs became stiffer and were successfully used to feed the FDM printer. Water removal was slow when carried out passively in a controlled atmosphere (desiccator) or accelerated by using active drying methods (heat or microwave). Pre-drying of the PRX/excipients and/or PMs did not show any positive effect on the printability of the FIL. On the contrary, dry heat and, preferably, microwave mediated drying processes were shown to reduce the holding time required for successful FDM printing, enabling on-demand production at the point of care.

The manufacture of medicines on demand for a particular patient, at the point of care, may be achieved via 3D printing, improving therapeutic outcomes, medication adherence and patient safety. Tablets are often printed using a combination of hot-melt extrusion and fused deposition modelling. In this work, paracetamol-loaded hydroxypropylcellulose filaments were produced; their extrudability and printability were aided by a plasticizer and a lubricant. For printability, 11% humidity was the ideal storage condition for filaments up to 6 months. The tablets produced complied with the uniformity of mass and content requirements, and showed delayed drug release; these characteristics were maintained after in-use stability testing for 30 days.

This work presents the preliminary development of paroxetine-based formulations containing hydroxypropylcellulose (HPC) polymers suitable for hot-melt extrusion coupled to fused deposition modeling (3D printing). Two grades of HPC (54% w/w), KlucelTM LF and KlucelTM GF, were tested in a polymeric formulation of paroxetine (30% w/w) and adjuvants (16% w/w of dicalcium dihydrate phosphate, magnesium stearate, and triethylcitrate; 10:1:5 ratio). Both formulations exhibited a release of almost 100% of paroxetine after 12 h, but the drug released from the KlucelTM LF formulation was quicker and closer to the formulations available in the market.

Species of the Diospyros L. genus (Ebenaceae family) have been largely used in traditional medicine for the treatment of several diseases, especially infectious ones. To date, active major compounds such as naphthoquinones, triterpenoids, and tannins have been isolated and pharmacologically validated from Diospyros species. The present study summarizes the information available in the literature on the species described in the Flora of Mozambique. To do so, scientific databases (e.g., PubMed, Scopus, Web of Science, and Google Scholar) were searched using various keywords and Boolean connectors to gather and summarize the information. Of the 31 native and naturalized species in the Flora of Mozambique, 17 are used in different regions of Africa and were described for their traditional uses. They were reported to treat more than 20 diseases, mostly infectious, in the gastrointestinal and oral cavity compartments. This work provides an overview of the therapeutical potential of Diospyros species and explores novel insights on the antimicrobial potential of extracts and/or isolated compounds of these Mozambican species.

Diazepam (DZP) is a long-acting benzodiazepine to treat anxiety or acute alcohol withdrawal. Although this class of drugs should be taken for a short period of time, many patients take them for longer than recommended, which has been linked to an increased risk of dementia and dependence. The present work aimed at using the dual-nozzle system of fused deposition modeling (FDM) 3D printers to prepare tablets with gradual doses of DZP with constant mass and size. Placebo and DZP-loaded filaments were prepared by hot-melt extrusion and used to print the bi-compartmental tablets. Thermal processing allowed the conversion of crystalline DZP to its amorphous counterpart. Tablets with different DZP contents were effectively printed with a mass, thickness and diameter average of 111.6 mg, 3.1 mm, and 6.4 mm, respectively. Microscopic data showed good adhesion between the different layers in the printed tablets. The desired drug contents were successfully achieved and were within the acceptance criteria (European Pharmacopeia). The combination of a placebo and drug-loaded extrudates proved to be beneficial in the production of tablets by FDM for patients in need of drug withdrawal.

Diospyros villosa L. (De Winter) (Ebenaceae) is a shrub whose root (DVR) is used as a toothbrush and to treat oral infections in Mozambique. The present work aims at establishing monographic quality criteria to allow the sustainable and safe development of pharmaceutical preparations with this herbal drug. This includes setting botanical (qualitative and quantitative) and chemical identification parameters, purity tests (loss on drying and total ash), quantifying the major classes of constituents identified, and particle size characterization of the powdered drug. DVR samples are cylindrical and microscopically characterized by: a periderm, with six layers of flattened phellem cells, with slightly thickened walls and few layers of phelloderm; cortical parenchyma with brachysclereids with a short, roughly isodiametric form (13.82–442.14 μm2 × 103), surrounded by a ring of prismatic calcium oxalate crystals; uniseriate medullary rays and prominent vessels of the xylem with single or double shape; numerous single and clustered starch grains, within the cortical parenchyma, medullar parenchyma, and ray cells. Polyphenols, mainly hydrolyzable tannins (212.29 ± 0.005 mg gallic acid equivalent/g of dried DVR), are the main marker class of constituents. Furthermore, the average diameter of the particles of the powder, 0.255 mm, allows its classification as a fine powder.

In situ amorphization is a promising approach, considered in the present work, to enhance the solubility and dissolution rate of olanzapine, while minimizing the exposure of the amorphous material to the stress conditions applied during conventional processing. The production of pellets by extrusion/spheronization and the coating of inert beads were investigated as novel methods to promote the co-amorphization of olanzapine, a poorly water-soluble drug, and saccharin. Samples were characterized using differential scanning calorimetry, X-ray powder diffraction, Fourier-transform infrared spectroscopy and scanning electron microscopy, and dissolution and stability testing. The co-amorphous produced were compared with crystalline olanzapine, or physical mixture of olanzapine and saccharin. Results suggested that the addition of water to mixtures containing olanzapine and saccharin during the production of pellets, and the coating of inert beads, induced the in situ co-amorphization of these substances. The coating of inert beads enhanced the solubility and dissolution rate of olanzapine, especially when compared to pellets coated with the crystalline drug, but also with pellets containing the co-amorphous entity in the matrix of beads. Nine months stability tests (23 °C/60% RH) confirmed the preservation of the solid-state properties of the co-amorphous form on/in pellets. Overall, results highlighted the feasibility and benefits of in situ co-amorphization, either when the drug was entrapped in the pellets matrix, or preferentially applied directly on the surface of pellets.

Individualised medicine demands the formulation of pharmacotherapy in accordance with the characteristics of each patient’s health condition, and paediatrics is one of the areas that needs this approach. The 3D printing of oral doses is one method for achieving customised medicine in paediatrics. In this work, pre-formulation studies were conducted to evaluate the viability of using specific raw materials to produce 3D printed dosage forms based on two active pharmaceutical ingredients (APIs), ondansetron and esomeprazole, which are important for therapeutic customisation in paediatrics. Pre-formulation studies were carried out by characterising the physical and chemical properties of selected raw materials, selected APIs and their mixtures, using analytical methods such as scanning electron microscopy (SEM), X-ray powder diffraction (X-RPD), simultaneous thermal analysis (STA) and differential scanning calorimetry (DSC). The flowability of powders, compatibility and stability studies were also performed. Among all the ingredients selected, the PVPs (K17, K25 and K90) had the best characteristics to incorporate both forms of Esomeprazole Mg in a formulation to produce extrudates. The results obtained validated the use of some selected raw materials for tablet manufacture by the 3D printing approach.

The work evaluates the stability of amorphous and co-amorphous olanzapine (OLZ) in tablets manufactured by direct compression. The flowability and the compressibility of amorphous and co-amorphous OLZ with saccharin (SAC) and the properties of the tablets obtained were measured and compared to those of tablets made with crystalline OLZ. The flowability of the amorphous and mostly of the co-amorphous OLZ powders decreased in comparison with the crystalline OLZ due to the higher cohesiveness of the former materials. The stability of the amorphous and co-amorphous OLZ prior to and after tableting was monitored by XRPD, FTIR, and NIR spectroscopies. Tablets presented long-lasting amorphous OLZ with enhanced water solubility, but the release rate of the drug decreased in comparison with tablets containing crystalline OLZ. In physical mixtures made of crystalline OLZ and SAC, an extent of amorphization of approximately 20% was accomplished through the application of compaction pressures and dwell times of 155 MPa and 5 min, respectively. The work highlighted the stability of amorphous and co-amorphous OLZ during tableting and the positive effect of compaction pressure on the formation of co-amorphous OLZ, providing an expedited amorphization technique, given that the process development-associated hurdles were overcome.

AbstractIntroduction Strategies to address the problem of poorly water-soluble drugs encompass the conversion of a crystalline drug into an amorphous form to promote its apparent solubility and dissolution. Co-amorphous systems (CAMs) incorporate low molecular mass molecules (co-formers), which are mixed with the drug to form one single phase [1,2]. The aim of this study is to understand the capability of different co-formers (amino, carboxylic and sulphonic acids), in the production of CAMs with olanzapine by ball milling, solvent evaporation and quench cooling.Materials and methods Mixtures (2 g) of olanzapine (OLZ) and each co-former [l-aspartate (ASP); l-tryptophan (TRY); l-arginine (ARG); l-proline (PRO); citric acid (CIT); tartaric acid (TAR); oxalic acid (OXA); saccharine (SAC); potassium acessulfame (ACE); cyclamic acid (CYC)] in 1:1 molar ratios were submitted to ball milling (BM), solvent evaporation (SE) and quench cooling (QC). CAMs were evaluated for the OLZ solubility increase, co-formability and storage stability over time, by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and Fourier-transform infra-red spectroscopy (FTIR).Results The BM technique presented the most promising results followed by QC and SE (Table 1), since more CAMs were produced. All the sulphonic acids (SAC, CYC and ACE) formed CAMs regardless of the technique used, presenting complete amorphization probably due to their higher ability to produce intermolecular interactions, like hydrogen-bonding, thus increasing the stability of CAMs (more than 8 weeks at 25 °C/11 and 53% RH). Conversely, amino acids were the least efficient in producing CAMs. Crystalline OLZ presented low solubility (40.1 mg/L) in water and a general increase in the solubility of the CAMs was observed. Carboxylic acids (TAR, CIT, OXA) achieved the biggest increase (up to 269 times, BM with TART) followed by sulphonic acids (up to 199 times, SE with SAC), unveiling the possibility of improved dissolution profiles and bioavailability. Discussion and conclusions: The study has shown the possibility of converting a crystalline drug into an amorphous entity, particularly when in presence of co-formers which stabilise the amorphous structures formed. In fact, with sulphonic acids, both SE and BM, achieved complete amorphization and successfully stabilised the CAMs obtained. Due to the noteworthy increase in solubility, resulting from co-amorphization, this technique is considered to be adequate to process active compounds with poor water solubility, such as OLZ.Table 1. Comparison of the of co-amorphization ability using different techniques and co-formers.[Table: see text]aIncomplete amorphization; bcomplete amorphization.

AbstractIntroduction The production of amorphous and co-amorphous (CAM) materials has been used as a procedure to overcome the poor water solubility shown by most of the drugs currently under development [1]. Ball milling has been considered to convert the crystalline state of a substance into its amorphous counterpart [2,3]. At present, the impact of the initial polymorphic form of a drug substance on its final amorphous state upon milling, has not been clearly studied. This work aims to compare the co-amorphization efficiency of two different polymorphic forms of olanzapine (OLZ; a BCS class II drug) using saccharin (SAC) as a co-former.Materials and methods OLZ (forms I and II) were the starting polymorphic forms to be milled with SAC (2:1 molar ratio). OLZ form I was used as received while OLZ form II was obtained from crystallisation of OLZ in dichloromethane. Ball milling was performed using 2.5 g of 3.0 mm Ø balls, for 2 h. The conversion of the crystalline states into the amorphous counterpart was monitored by calorimetry (DSC) and diffractometry (XRPD).Results The thermograms and the diffractograms obtained (Figure 1) have shown a clear difference between the final products of the two polymorphic forms of OLZ. XRPD peaks were less intense for OLZ form II and most representative of SAC, indicating that OLZ was indeed mostly converted into the amorphous state. On the other hand, when OLZ form I was the starting material, a richer diffractogram resulted, suggesting that a crystalline fraction of OLZ remained in the particles’ network of the final product, a feature also confirmed by DSC. Discussion and conclusions: Since OLZ form II has a higher thermodynamic energy than form I, it is not surprising that the former exhibits better amorphization ability. Thus, it is expected that either an increase on milling time, or milling speed, would enhance the co-amorphization of OLZ form I with SAC.[Figure: see text]

AbstractIntroduction A large number of active pharmaceutical compounds currently under development are poorly water soluble, which can limit their bioavailability and results in formulation challenges [1]. Co-amorphous systems (CAMs) are known to increase the apparent solubility and dissolution rate of drugs [1,2]. To date, sulphonic acids have never investigated as possible co-formers for Olanzapine (OLZ; a BSC class II drug) and, thus, the aim of this work is to evaluate their potential on the formation of stable CAMs.Materials and methods OLZ was used as model drug. Saccharin (SAC), cyclamic acid (CA), acesulfame (ACE; obtained by neutralisation of potassium acesulfame) and their salts, sodium saccharin, sodium cyclamate and potassium acesulfame, respectively, were used as co-formers. Mixtures (2 g) of OLZ and each co-former, in molar ratios 1:1, were submitted to milling, solvent evaporation (SE) and quench cooling. Samples were characterised by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Fourier-transform infra-red spectroscopy (FTIR) and cooling/heating stage microscopy. Solubility assessment, powder dissolution rate and stability studies were also performed.Results SAC, CA and ACE demonstrated to be successful co-formers in the production and stabilisation of OLZ-CAMs obtained by the three different techniques, presenting a single glass transition temperature (Tg) in thermograms and a typical halo in XRPD diffractograms. None of the salts were capable of forming a CAM, resulting in phase separation and absence of Tg events. Microscopical analysis supported DSC data and provided images of the CAMs recrystallization. Band shifts and broadening of the CAMs FTIR spectra suggest an intermolecular interaction between the N–H group in OLZ and the C = O group in SAC and ACE and the O-H group in CA. Solubility of OLZ was significantly increased (up to 199 times) when produced by SE with SAC. Dissolution rate was also increased for all the CAMs produced. SAC and CA successfully stabilised the CAMs produced, for more than 8 weeks at 25 °C/11, 53 and 75% RH and at 25 °C/11 and 53% RH, respectively.Discussion and conclusions In this study OLZ was successfully amorphized using the neutral forms of the sulphonic acids. The impossibility of the salts to form a CAM is in agreement with the FTIR results, since the groups responsible for the molecular interaction with OLZ are unavailable in these molecules due to their negative charge. SE proved to be the best technique to produce CAMs with the different co-formers, resulting in the highest increase in solubility. SAC has shown to be the best co-former, with the highest solubility and stability over time, under higher relative humidity. Moreover, the increased dissolution rate of the CAMs suggests improved bioavailability of OLZ, a feature with therapeutic impact, which should be confirmed in vivo.

AbstractIntroduction Amorphous and co-amorphous (CAM) materials have recently been used to improve oral bioavailability of drugs, by enhancing water solubility and dissolution rate from solid dosage forms [1,2]. However, stress conditions imposed on amorphous systems during production of such dosage forms (e.g. pressure upon tableting), can revert the drug back into the less soluble crystalline form [3]. This work thus presents a methodology to monitor and quantify the fraction of amorphous olanzapine (OLZ) remaining in immediate release OLZ tablets (Table 1).Table 1. Predicted fraction of amorphous OLZ, by NIR and FTIR spectroscopies, in tablets prepared with the co-amorphous system.[Table: see text]Materials and methods Near infra-red (NIR, 9000–4000 cm−1) and Fourier-transform infra-red (FTIR, 4000–500 cm−1) techniques were used to quantify the fraction of co-amorphous OLZ (30%) with saccharin (SAC; 18%) in formulations containing also calcium phosphate (27%), microcrystalline cellulose (20%) and povidone (5%). Tablets (250 mg) were obtained using a universal testing machine fit with circular punches (7.5 mm Ø), at a constant compression rate of 10 mm/min (n = 5); different compression forces (8 and 25 kN) and dwell times (DT; 0 and 20 min) were considered. Evaluation of the impact of the compression conditions on the recrystallization of OLZ from a co-amorphous system was based on a computational model.Results Using a 2nd derivative filter to process both NIR and FTIR spectra, the quantification of amorphous olanzapine was possible with a root mean square error of calibration and prediction above 2% (Figure 1). The method was further applied to evaluate the stability of co-amorphous systems after tableting, revealing that no significant recrystallization occurred, i.e. the co-amorphous were stable under the stress conditions applied. Discussion and conclusions: The use of NIR and FTIR resulted in high correlation between the predicted values and the expected ones, thus enabling these spectroscopic techniques to be used to monitor the conversion of amorphous into crystalline OLZ forms and thus estimate the impact on drug bioavailability. Understanding of the conversion kinetics will ultimately allow anticipation of the time for complete recrystallization. The model developed has also demonstrated that tablets produced were stable, since no recrystallization was observed.[Figure: see text]

The use of physiologically based pharmacokinetic (PBPK) models to support drug product development has become increasingly popular. The in vitro characterization of the materials of the formulation provides valuable descriptors for the in silico prediction of the drug’s pharmacokinetic profile. Thus, the application of an in vitro–in silico framework can be decisive towards the prediction of the in vivo performance of a new medicine. By applying such an approach, this work aimed to derive mechanistic based insights into the potential impact of carrier particles and powder bulk properties on the in vivo performance of a lactose-based dry powder inhaler (DPI). For this, a PBPK model was developed using salbutamol sulphate (SS) as a model drug and the in vitro performance of its low-dose blends (2% w/w) with different types of lactose particles was investigated using different DPI types (capsule versus reservoir) at distinct airflows. Likewise, the influence of various carrier’s particle and bulk properties, device type and airflow were investigated in silico. Results showed that for the capsule-based device, low-dose blends of SS had a better performance, when smaller carrier particles (Dv0.5 ≈ 50 μm) with about 10% of fines were used. This resulted in a better predicted bioavailability of the drug for all the tested airflows. For the reservoir type DPI, the mean particle size (Dv0.5) was identified as the critical parameter impacting performance. Shear cell and air permeability or compressibility measurements, particle size distribution by pressure titration and the tensile strength of the selected lactose carrier powders were found useful to generate descriptors that could anticipate the potential in vivo performance of the tested DPI blends.

The data presented in this article are related to the production of 1:1 Caffeine:Glutaric Acid cocrystals as part of the research article entitled “Green production of cocrystals using a new solvent-free approach by spray congealing” (Duarte et al., 2016) [1]. More specifically, here we present the thermal analysis and the X-ray powder diffraction data for pure Glutaric Acid, used as a raw material in [1]. We also include the X-ray powder diffraction and electron microscopy data obtained for the 1:1 Caffeine:Glutaric Acid cocrystal (form II) produced using the cooling crystallization method reported in “Operating Regions in Cooling Cocrystallization of Caffeine and Glutaric Acid in Acetonitrile” (Yu et al., 2010) [2]. Lastly, we show the X-ray powder diffraction data obtained for assessing the purity of the 1:1 Caffeine:Glutaric cocrystals produced in [1].

Three-dimensional (3D) printing offers the greatest potential to revolutionize the future of pharmaceutical manufacturing by overcoming challenges of conventional pharmaceutical operations and focusing design and production of dosage forms on the patient’s needs. Of the many technologies available, fusion deposition modelling (FDM) is considered of the lowest cost and higher reproducibility and accessibility, offering clear advantages in drug delivery. FDM requires in-house production of filaments of drug-containing thermoplastic polymers by hot-melt extrusion (HME), and the prospect of connecting the two technologies has been under investigation. The ability to integrate HME and FDM and predict and tailor the filaments’ properties will extend the range of printable polymers/formulations. Hence, this work revises the properties of the most common pharmaceutical-grade polymers used and their effect on extrudability, printability, and printing outcome, providing suitable processing windows for different raw materials. As a result, formulation selection will be more straightforward (considering the characteristics of drug and desired dosage form or release profile) and the processes setup will be more expedite (avoiding or mitigating typical processing issues), thus guaranteeing the success of both HME and FDM. Relevant techniques used to characterize filaments and 3D-printed dosage forms as an essential component for the evaluation of the quality output are also presented.

Currently, insulin can only be administered through the subcutaneous route. Due to the flaws associated with this route, it is of interest to orally deliver this drug. However, insulin delivered orally has several barriers to overcome as it is degraded by the stomach’s low pH, enzymatic content, and poor absorption in the gastrointestinal tract. Polymers with marine source like chitosan are commonly used in nanotechnology and drug delivery due to their biocompatibility and special features. This work focuses on the preparation and characterization of mucoadhesive insulin-loaded polymeric nanoparticles. Results showed a suitable mean size for oral administration (

Pancreatic cancer is the eighth leading cause of cancer death worldwide. For this reason, the development of more effective therapies is a major concern for the scientific community. Accordingly, plants belonging to Plectranthus genus and their isolated compounds, such as Parvifloron D, were found to have cytotoxic and antiproliferative activities. However, Parvifloron D is a very low water-soluble compound. Thus, nanotechnology can be a promising delivery system to enhance drug solubility and targeted delivery. The extraction of Parvifloron D from P. ecklonii was optimized through an acetone ultrasound-assisted method and isolated by Flash-Dry Column Chromatography. Then, its antiproliferative effect was selectivity evaluated against different cell lines (IC50 of 0.15 ± 0.05 μM, 11.9 ± 0.7 μM, 21.6 ± 0.5, 34.3 ± 4.1 μM, 35.1 ± 2.2 μM and 32.1 ± 4.3 μM for BxPC3, PANC-1, Ins1-E, MCF-7, HaCat and Caco-2, respectively). To obtain an optimized stable Parvifloron D pharmaceutical dosage form, albumin nanoparticles were produced through a desolvation method (yield of encapsulation of 91.2%) and characterized in terms of size (165 nm; PI 0.11), zeta potential (−7.88 mV) and morphology. In conclusion, Parvifloron D can be efficiently obtained from P. ecklonii and it has shown selective cytotoxicity to pancreatic cell lines. Parvifloron D nanoencapsulation can be considered as a possible efficient alternative approach in the treatment of pancreatic cancer.