Development and Evaluation of a Stable Oil-in-Water Emulsion with High Ostrich Oil Concentration for Skincare Applications.

This study investigates the development of an oil-in-water (O/W) emulsion enriched with a high concentration of ostrich oil, recognized for its abundant content of oleic acid (34.60 ± 0.01%), tailored for skincare applications. Using Span and Tween emulsifiers, we formulated an optimized emulsion with 20% w/w ostrich oil and a 15% w/w blend of Span 20 and Tween 80. This formulation, achieved via homogenization at 3800 rpm for 5 min, yielded the smallest droplet size (5.01 ± 0.43 µm) alongside an appropriate zeta potential (-32.22 mV). Our investigation into the influence of Span and Tween concentrations, types, and ratios on the stability of 20% w/w ostrich oil emulsions, maintaining a hydrophile-lipophile balance (HLB) of 5.5, consistently demonstrated the superior stability of the optimized emulsion across various formulations. Cytotoxicity assessments on human dermal fibroblasts affirmed the safety of the emulsion. Notably, the emulsion exhibited a 52.20 ± 2.01% inhibition of linoleic acid oxidation, surpassing the 44.70 ± 1.94% inhibition observed for ostrich oil alone. Moreover, it demonstrated a superior inhibitory zone against Staphylococcus aureus (12.32 ± 0.19 mm), compared to the 6.12 ± 0.15 mm observed for ostrich oil alone, highlighting its enhanced antioxidant and antibacterial properties and strengthening its potential for skincare applications. The optimized emulsion also demonstrates the release of 78.16 ± 1.22% of oleic acid across the cellulose acetate membrane after 180 min of study time. This successful release of oleic acid further enhances the overall efficacy and versatility of the optimized emulsion. Stability assessments, conducted over 6 months at different temperatures (4 °C, 25 °C, 45 °C), confirmed the emulsion's sustained physicochemical and microbial stability, supporting its promise for topical applications. Despite minor fluctuations in acid values (AV) and peroxide values (PV), the results remained within the acceptable limits. This research elucidates the crucial role of emulsification in optimizing the efficacy and stability of ostrich oil in skincare formulations, providing valuable insights for practical applications where stability is paramount.

Overcoming Solubility Challenges: Self-emulsifying Systems for Enhancing the Delivery of Poorly Water-Soluble Antiviral Drugs.

The primary goal of drug formulation is to improve a drug's bioavailability in the body. However, poorly water-soluble drugs present challenging issues related to their solubility and bioavailability factors. Emerging technologies, such as lipid-based drug delivery systems, including micro- or nanoemulsifying drug delivery systems, have become increasingly relevant to address the above challenges. This review presents a thorough overview of self-emulsifying drug delivery systems (SEDDS). It covers the properties, principles, self-emulsification mechanism, formulation strategies, and characterization methods of SEDDS. This review also addresses the delivery of antiviral agents through SEDDS. Moreover, it summarizes the marketed formulations of SEDDS consisting of antiviral agents. This review offers a comprehensive and valuable resource for future perspectives on SEDDS and their potential applications in antiviral drug delivery.

Fabrication and Optimization of Electrospun Shellac Fibers Loaded with Senna alata Leaf Extract.

Single-fluid electrospinning creates nanofibers from molten polymer solutions with active ingredients. This study utilized a combination of a fractional factorial design and a Box-Behnken design to examine crucial factors among a multitude of parameters and to optimize the electrospinning conditions that impact fiber mats' morphology and the entrapment efficiency of Senna alata leaf extract. The findings indicated that the shellac content had the greatest impact on both fiber diameter and bead formation. The optimum electrospinning conditions were identified as a voltage of 24 kV, a solution feed rate of 0.8 mL/h, and a shellac-extract ratio of 38.5:3.8. These conditions produced nanosized fibers with a diameter of 306 nm, a low bead-to-fiber ratio of 0.29, and an extract entrapment efficiency of 96% within the fibers. The biphasic profile of the optimized nanofibers was confirmed with an in vitro release study. This profile consisted of an initial burst release of 88% within the first hour, which was succeeded by a sustained release pattern surpassing 90% for the next 12 h, as predicted with zero-order release kinetics. The optimized nanofibers demonstrated antimicrobial efficacy against diverse pathogens, suggesting promising applications in wound dressings and protective textiles.

Nanoemulsion-Based Orodispersible Film Formulation of Guava Leaf Oil for Inhibition of Oral Cancer Cells.

Among natural sources, guava leaf oil (GLO) has emerged as a potential anticancer agent. However, its limited water solubility poses a significant challenge for its use. Oil-in-water nanoemulsions are used to address the limitation of water solubility of GLO prior to its incorporation into orodipersible films. Nanoemulsions containing GLO:virgin coconut oil (VCO) at a ratio of 50:50 to 70:30 presented a small droplet size of approximately 50 nm and a relatively low zeta potential. GLO:VCO at a ratio of 70:30 was selected for incorporation into sodium alginate film at various concentrations ranging from 1% to 30% w/w. Tensile strength and elongation at break relied on the concentration of nanoemulsions as well as the internal structure of films. Fourier transform infrared spectroscopy revealed that GLO was compatible with sodium alginate. Film containing 2% w/w of nanoemulsions (2G_ODF) exhibited effective in vitro antioral cancer activity, with an IC50 of 62.49 ± 6.22 mg/mL; furthermore, its anticancer activity showed no significant difference after storage at 25 °C for 1 year. Moreover, 2G_ODF at IC60 arrested colony formation and cell invasion. There is also evidence that cell death occurred via apoptosis, as indicated by nuclear fragmentation and positive Annexin-V staining. These findings highlight the potential of orodispersible films containing GLO nanoemulsions as a prospective oral anticancer agent.

Advances in Natural Product Extraction Techniques, Electrospun Fiber Fabrication, and the Integration of Experimental Design: A Comprehensive Review.

The present review explores the growing interest in the techniques employed for extracting natural products. It emphasizes the limitations of conventional extraction methods and introduces superior non-conventional alternatives, particularly ultrasound-assisted extraction. Characterization and quantification of bioactive constituents through chromatography coupled with spectroscopy are recommended, while the importance of method development and validation for biomarker quantification is underscored. At present, electrospun fibers provide a versatile platform for incorporating bioactive extracts and have extensive potential in diverse fields due to their unique structural and functional characteristics. Thus, the review also highlights the fabrication of electrospun fibers containing bioactive extracts. The preparation of biologically active extracts under optimal conditions, including the selection of safe solvents and cost-effective equipment, holds promising potential in the pharmaceutical, food, and cosmetic industries. Integration of experimental design into extraction procedures and formulation development is essential for the efficient production of health products. The review explores potential applications of encapsulating natural product extracts in electrospun fibers, such as wound healing, antibacterial activity, and antioxidant properties, while acknowledging the need for further exploration and optimization in this field. The findings discussed in this review are anticipated to serve as a valuable resource for the processing industry, enabling the utilization of affordable and environmentally friendly, natural, and raw materials.

Controlled Release of Felodipine from 3D-Printed Tablets with Constant Surface Area: Influence of Surface Geometry.

In this study, 3D-printed tablets with a constant surface area were designed and fabricated using polylactic acid (PLA) in the outer compartment and polyvinyl alcohol and felodipine (FDP) in the inner compartment. The influences of different surface geometries of the inner compartment, namely, round, hexagon, square, and triangle, on drug release from 3D-printed tablets were also studied. The morphology and porosity of the inner compartment were determined using scanning electron microscopy and synchrotron radiation X-ray tomographic microscopy, respectively. Additionally, drug content and drug release were also evaluated. The results revealed that the round-shaped geometry seemed to have the greatest total surface area of the inner compartment, followed by square-shaped, hexagon-shaped, and triangle-shaped geometries. FDP-loaded 3D-printed tablets with triangle and hexagon surface geometries had the slowest drug release (about 80% within 24 h). In the round-shaped and square-shaped 3D-printed tablets, complete drug release was observed within 12 h. Furthermore, the drug release from triangle-shaped 3D-printed tablets with double the volume of the inner compartment was faster than that of a smaller volume. This was due to the fact that a larger tablet volume increased the surface area contacting the medium, resulting in a faster drug release. The findings indicated that the surface geometry of 3D-printed tablets with a constant surface area affected drug release. This study suggests that 3D printing technology may be used to develop oral solid dosage forms suitable for customized therapeutic treatments.

Preparation of Bioactive De-Chlorophyll Rhein-Rich Senna alata Extract.

Senna alata leaves display various biological activities as a result of their rhein and phenolic composition. The objective of this study was to develop bioactive de-chlorophyll rhein-rich S. alata extracts. The rhein content was quantified using a validated high-performance liquid chromatography-diode array detection (HPLC-DAD) method. The best process parameters for maximizing rhein were established using ultrasound-assisted extraction (UAE). The optimal conditions for the parameters were determined using the Box-Behnken design (BBD); 95% v/v ethanol was used as the extraction solvent at 59.52 °C for 18.4 min with a solvent-to-solid ratio of 25.48:1 (mL/g) to obtain the predicted value of rhein at 10.44 mg/g extract. However, the color of the rhein-rich extract remained dark brown. For the removal of chlorophyll, liquid-liquid extraction with vegetable oils and adsorption with bleaching agents were employed. The bleaching agents were significantly more effective at removing chlorophyll and had less of an effect on the reduction in rhein content than vegetable oils. The presence of rhein and phenolics in the de-chlorophyll extracts might be responsible for their antioxidant, anti-inflammatory, and antibacterial activities. These findings indicate that rhein-rich extract and its de-chlorophyll extracts possess sufficient biological activities for the further development of cosmeceuticals and pharmaceuticals.

Design and development of 3D-printed bento box model for controlled drug release of propranolol HCl following pharmacopeia dissolution guidelines.

The goal of this study was to develop a 3D-printed bento box model (3D-printed BB) with one or two chambers containing propranolol hydrochloride (PNL) as powder and matrix tablet for controlled drug release at varying times using United States Pharmacopeia (USP) dissolution guidelines. The 3D-printed BBs were made with commercial polyvinyl alcohol filament and a fused deposition modeling (FDM) 3D printer, with varying infill percentages and wall thicknesses. The physicochemical properties of the 3D-printed BBs, including appearance, thickness, size, weight, hardness, swelling, and erosion properties were investigated. The surface and cross-section morphologies of the 3D-printed BBs were characterized using a FESEM. According to FESEM images, the different infill percentages had a significant effect on the internal structure of the 3D-printed BBs' caps, but a minor effect on the internal structure of their walls. PNL release from the 3D-printed BB began in a pH 1.2 medium, followed by drug release in a pH 6.8 medium. Some formulations of 3D-printed BB could achieve a drug release percentage within all the ranges specified by USP dissolution guidelines. 3D-printed BBs, therefore, have the potential to revolutionize the future of the pharmaceutical industry by facilitating control of the amount of drugs released at predetermined intervals.

New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method.

Quercetin (QCT), a natural flavonoid, is of research interest owing to its pharmacological properties. However, its pharmacokinetic limitations could hinder its widespread therapeutic use. Nanocarriers, especially solid lipid nanoparticles (SLNs), might overcome this constraint. This study aimed to investigate QCT-loaded SLNs prepared via a new approach using a volatile oil. The phase-inversion temperature method was used to incorporate rosemary oil (RMO) into SLNs prepared using solid lipids possessing different chemical structures. Among the solid lipids used in the formulations, trilaurin (TLR) exhibited the smallest particle size and good stability after a temperature cycling test. SLNs prepared with a ratio of RMO to TLR of 1:3 could load QCT with an entrapment efficiency of >60% and drug loading of ~2% w/w. The smallest particle size was achieved using the polyoxyethylene-hydrogenated castor oil RH40, and the particle size depended on the concentration. The drug-release profile of QCT_TLR exhibited prolonged biphasic release for >24 h. QCT_TLR was a safe formulation, as indicated by a cell viability percentage of >75% at <2% v/v. In a computer simulation, the system with RMO enabled smaller sized SLNs than those without RMO. This new discovery shows great promise for producing SLNs via the phase-inversion temperature method with incorporation of volatile oil, particularly for delivering compounds with limited water solubility.

Optimization of Ultrasound-Assisted Extraction of Yields and Total Methoxyflavone Contents from Kaempferia parviflora Rhizomes.

The major bioactive components of Kaempferia parviflora (KP) rhizomes, 3,5,7,3',4'-pentamethoxyflavone (PMF), 5,7-dimethoxyflavone (DMF), and 5,7,4'-trimethoxyflavone (TMF), were chosen as the quantitative and qualitative markers for this plant material. In order to extract bioactive components (total methoxyflavones) from KP rhizomes, ultrasound-assisted extraction (UAE) was proposed as part of this study. Plackett-Burman design (PBD) and Box-Behnken design (BBD) were utilized to optimize the effects of UAE on extraction yields and total methoxyflavone contents in KP rhizomes. First, PBD was utilized to determine the effect of five independent variables on total yields and total methoxyflavone contents. The results indicated that the concentration of the extracting solvent (ethanol), the extraction time, and the ratio of solvent to solid were significant independent terms. Subsequently, BBD with three-level factorial experiments was used to optimize the crucial variables. It was discovered that the concentration of ethanol was the most influential variable on yields and total methoxyflavone contents. Optimum conditions for extraction yield were ethanol concentration (54.24% v/v), extraction time (25.25 min), and solvent-to-solid ratio (49.63 mL/g), while optimum conditions for total methoxyflavone content were ethanol concentration (95.00% v/v), extraction time (15.99 min), and solvent-to-solid ratio (50.00 mL/g). The relationship between the experimental and theoretical values was perfect, which proved that the regression models used were correct and that PBD and BBD were used to optimize the conditions in the UAE to obtain the highest yield and total methoxyflavone content in the KP rhizomes.

Impact of Fixed Oil on Ostwald Ripening of Anti-Oral Cancer Nanoemulsions Loaded with Amomum kravanh Essential Oil.

Recently, essential oil from Amomum kravanh (AMO) was reported to exert anti-oral cancer effects. Although it was more effective after being loaded into nanoemulsions, AMO without an Ostwald ripening inhibitor was unable to form stable nanoemulsions because of the Ostwald ripening phenomenon. In this study, we examined the influence of Ostwald ripening inhibitors, such as fixed oils and polyethylene glycol 4000 (PEG 4000), on nanoemulsion properties prepared by a phase inversion temperature method. Several fixed oils, including virgin coconut oil (VCO), palm oil (PMO), olive oil (OLO), and PEG 4000, were evaluated, and their Ostwald ripening inhibitory effects were compared. The results suggest that the type and ratio of AMO:fixed oils influence the formation and characteristics of nanoemulsions. PEG 4000 was unable to produce nanoemulsions; however, stable nanoemulsions with small droplet sizes were observed in preparations containing OLO and VCO at an AMO:fixed oil ratio of 80:20, which may be the result of specific molecular interactions among the components. Using an MTT assay, we demonstrated that the AMO:OLO (80:20) nanoemulsion produced the most significant cytotoxic effect on oral cancer cells with a percentage of 99.68 ± 0.56%. Furthermore, the AMO:OLO 80:20 nanoemulsion inhibits metastasis and induces oral cancer cell death through the intrinsic apoptosis pathway. In conclusion, AMO nanoemulsion with anti-oral cancer activity was successfully produced by varying the amount and type of fixed oils. In the future, this discovery may lead to the development of stable nanoemulsions employing additional volatile oils.

Monolaurin-Loaded Gel-Like Microemulsion for Oropharyngeal Candidiasis Treatment: Structural Characterisation and In Vitro Antifungal Property.

Recently, monolaurin (ML) has received great interest due to its possible use as an alternative antifungal. However, the limited water solubility of ML is still a major obstacle to its formulation and application. Gel-like microemulsions are one of the promising carriers for low-water-solubility substances due to both the advantages of gels and microemulsions and may be applied for ML. In this study, ML was incorporated into gel-like microemulsions and evaluated for its physicochemical and antifungal properties. The results indicated that the properties of gel-like microemulsion changed after the incorporation of ML, suggesting that ML can induce the transition of internal structure. When simulating the oral cavity environment, changes in the microstructure were observed and depended on the times of dilution. The lamellar structure was formed at 1.5-2 times dilution. However, this structure was disrupted after dilution five times or more. The structural change following dilution was associated with the release profiles. After contacting the formulations with the medium, ML was promptly released, with the majority of ML being released within 2 h. Regarding the antifungal assay, the ML-loaded gel-like microemulsions decreased the survival of Candida albicans within 3 h, although ML was immediately released, suggesting that the ML-loaded in oil droplets required time to permeate through the fungal cell wall. Additionally, the gel-like microemulsions possessed acceptable stability after the temperature cycling test. Therefore, gel-like microemulsions can be a possible carrier for ML loading, and ML-loaded gel-like microemulsions may be applied as an alternative antifungal preparation in the future. Graphical abstract.

Chitosan film containing antifungal agent-loaded SLNs for the treatment of candidiasis using a Box-Behnken design.

The aim of this study was to combine fluconazole (FZ)-loaded solid lipid nanoparticles (FZ-SLNs) and chitosan films (C-films) for the potential administration of FZ across the buccal mucosa using a Box-Behnken design. The chitosan films containing FZ-SLNs (C-FS-films) and C-films were prepared using a film casting method. The ATR-FTIR analysis confirmed the presence of hydrogen bonds between the NH3+ groups of chitosan and the OH or COO- groups of glyceryl monostearate in the films. Additionally, FESEM analysis of the morphology of C-FS-films revealed the presence of FZ-SLNs in the films. Permeation studies using porcine buccal mucosa demonstrated that FZ from the C-FS-films was more permeable than in C-films. The antifungal activity of the C-FS-films was evaluated against Candida albicans, and inhibition zones were observed. Thus, C-FS-films represent an exciting drug carrier for the treatment of candidiasis via the buccal mucosa.

Fabrication, Optimization, and Characterization of Antibacterial Electrospun Shellac Fibers Loaded with Kaempferia parviflora Extract.

This study aimed to develop a Kaempferia parviflora (KP) extract based on electrospun shellac fibers capable of transporting methoxyflavones. This study used a Box-Behnken design to determine the optimal production parameters that influence the fiber diameter and bead-to-fiber ratio responses. The optimization step produced fibers with a small diameter (574 nm) and a lower bead-to-fiber ratio (0.48 beads per fiber) by combining 37.25% w/w shellac and 1.50% w/w KP extract with a solution feed rate of 0.8 mL/h and an electrical voltage of 18 kV. The KP extract was found to be dispersed throughout the electrospun shellac fibers during the characterization study. The results were highly correlated with the theoretical values, indicating that the regression models used to predict the response variables were adequate. A study of in vitro dissolution confirmed that KP extract-loaded electrospun shellac fibers could produce a sustained-release profile within 10 h. Additionally, KP-infused shellac fibers demonstrated antibacterial activity against Staphylococcus aureus. This KP loading method combined with shellac properties provided a new delivery system and could be used to explore novel biomedical materials.

Improvement of Bleached Shellac as Enteric Coating by Composite Formation.

The objective of this study was to stabilize the enteric property of bleached shellac by composite formation with ethyl cellulose. The composite film at the ratio of 9:1, 8:2, 7:3, 6:4, and 5:5 was prepared by the film casting method. The physicochemical properties were acid value, insoluble solid, water permeability coefficient, % polarity, mechanical property, FTIR, PXRD, DSC, % solubility in aqueous, and various pH (1.2 and 7.4). All the films were able to protect against the low pH and water. The total solubility at pH 7.4 was reported for the low ratio of ethyl cellulose (9:1 and 8:2). The stability of all films was then investigated for 180 days. The results demonstrated that the ethyl cellulose could stabilize the bleached shellac indicated by the low changes in acid value and insoluble solid. The higher ratio of ethyl cellulose contributed to the lower polymerization during storage. The results were due to the protection of the bleached shellac's active sites. The entanglement of ethyl cellulose caused interaction difficulties between active groups leading to stabilized bleached shellac. The proper ratio was 7:3 because of high solubility, and low polymerization. The findings demonstrated that the composite film could improve the enteric property of bleached shellac for a long period.

Preparation and characterization of triamterene complex with ascorbic acid derivatives.

The purpose of this study was to prepare solid dispersions of triamterene (TRT) with ascorbic acid (AA) or ascorbic acid 2 glucoside (AA2G) and to evaluate their physical properties. Solid dispersions were prepared by dissolving each sample in an organic solvent and evaporation (EVP). Powder X-ray diffraction (PXRD) revealed a halo pattern for EVP1 (AA/TRT = 1/1) and EVP2 (AA2G/TRT = 1/1). In differential scanning calorimetry (DSC), endothermic peaks due to the melting of TRT and AA disappeared for EVP1 (AA/TRT = 1/1), and the melting peaks of TRT and AA2G disappeared for EVP2 (AA2G/TRT = 1/1). Fourier transform infrared (FT-IR) spectroscopy revealed broadened peaks for EVP1 (AA/TRT = 1/1) and EVP2 (AA2G/TRT = 1/1) due to the hydroxyl groups (-OH) of AA and the amino groups (-NH2) of TRT and also revealed a peak shift due to the pteridine skeleton (C = N) of TRT. In near-infrared absorption (NIR) spectroscopy, peaks due to the hydroxyl groups (-OH) of AA and AA2G were found for EVP1 (AA/TRT = 1/1) and EVP2 (AA2G/TRT = 1/1), respectively. A peak due to the amino groups (-NH2) was evident. This suggested the formation of an evaporation, in which TRT interacted with AA or AA2G. In the dissolution test, the dissolved fraction of TRT alone after 3 min was 30%, whereas the fractions were enhanced to approximately 90% for EVP1 (AA/TRT = 1/1) and EVP2 (AA2G/TRT= 1/1). Results confirmed that dissolution properties were improved as a result of complex formation. The above findings indicated improvement the dissolution properties of TRT.

Phytochemical analysis of baby corn silk extracts.

BACKGROUND: Baby corn silk extract can be used as an antioxidant dietary supplement. However, insufficient data exists for this extract to guarantee its quality, efficacy and safety. OBJECTIVE: To determine phytochemical constituents, contents of phenolics and flavonoids, antioxidant activities, heavy metal concentrations, and microbial contamination of baby corn silk extracts. MATERIAL AND METHODS: Baby corn silks including Pacific 271 and Zeba SG 17 hybrids were individually extracted with 40% v/v ethanol and distilled water to obtain Pacific 271 ethanol extract (PE), Zeba SG 17 ethanol extract (ZE), Pacific 271 aqueous extract (PA), and Zeba SG 17 aqueous extract (ZA). The analysis of phytochemical constituents was carried out using phytochemical tests, TLC screening, UV-visible, FTIR, and 1H NMR experiments. The contents of phenolics and flavonoids were determined using the modified Folin-Ciocalteu and aluminium chloride colorimetric procedures, respectively. Antioxidant activities were investigated using DPPH and FRAP assays. The concentrations of heavy metals were analyzed by ICP-MS. Microbial enumeration tests were carried out according to the United States Pharmacopeia (USP) 41. RESULTS: PE and ZE were composed of flavonoids, tannins, terpenoids, and steroids while PA and ZA contained flavonoids and tannins. PE and ZE exhibited higher total phenolic and flavonoid contents and significantly stronger antioxidant activities than PA and ZA. All extracts conformed to the microbiological and heavy metal requirements according to Association of South East Asian Nations (ASEAN) guidelines. CONCLUSION: PE and ZE were considered appropriate to use as natural extracts of phenolics and flavonoids with antioxidant activities and safety.

Design and characterisation of electrospun shellac-polyvinylpyrrolidone blended micro/nanofibres loaded with monolaurin for application in wound healing.

Due to their ultrafine network structures, electrospun nanofibres have been potentially used for wound application. In order to develop a desired wound dressing material, shellac (SHL) was blended with polyvinyl pyrrolidone (PVP). Monolaurin (ML), which is a natural antimicrobial lipid, was incorporated into the SHL-PVP blended fibres to prevent delayed wound healing resulting from microbial infection. A full factorial design with three replicated centre points was employed in order to determine the main and interaction effects of various factors including SHL ratio in SHL-PVP blended solution, ML content and applied voltage on the multiple responses such as morphology, surface wettability, absorbency and mechanical properties. According to the results, an increase in the PVP content could lead to a significant increase in tensile strength and elongation. In addition, the presence of PVP contributed to an improvement in the drug loading capacity and dissolution rate. The fabricated fibres loaded with ML exhibited an excellent activity against Staphylococcus aureus and Candida albicans, and also provided an enhanced ability in the cell adhesion. Therefore, SHL-PVP blended fibres loaded with ML might be effectively used for application in wound healing.

Optimization and comparison of GC-FID and HPLC-ELSD methods for determination of lauric acid, mono-, di-, and trilaurins in modified coconut oil.

Modified coconut oil (MCO) obtained from the glycerolysis of virgin coconut oil (VCO) and glycerol under various conditions should have different amounts of bioactive fatty acids (FAs) and acylglycerols (AGs). Methods were developed to analyze lauric acid (LA), monolaurin (ML), dilaurin (DL), and trilaurin (TL) in MCO samples using gas chromatography - flame ionization detector (GC-FID) and high performance liquid chromatography - evaporative light scattering detector (HPLC-ELSD). The purpose of this research is to optimize and compare GC-FID and HPLC-ELSD methods for determination of LA, ML, DL, and TL in MCO samples. All the standard curves exhibited good linearity (R2 ≥ 0.9995), except for that of LA analyzed by HPLC-ELSD (R2 = 0.9971). The limits of detection (LODs) and quantification (LOQs) were found to be in the range of 0.033-0.260 mg/ml and 0.099-0.789 mg/ml for the GC-FID method and 0.040-0.421 mg/ml and 0.122-1.277 mg/ml for the HPLC-ELSD method, respectively. The GC-FID method (LOD ≤ 0.033 mg/ml) was more sensitive than HPLC-ELSD method (LOD ≤ 0.421 mg/ml) and showed satisfactory recoveries for LA analysis while HPLC-ELSD method (LOD ≤ 0.040 mg/ml) was more sensitive than GC-FID method (LOD ≤ 0.260 mg/ml) and exhibited acceptable recoveries for TL analysis. Both methods were applied to determine the MCO samples produced under varied conditions for glycerolysis. The results revealed that the developed GC-FID method is suitable for the quantification of LA, ML, and DL while the developed HPLC-ELSD method is appropriate for the determination of ML, DL, and TL. Both developed GC-FID and HPLC-ELSD methods produced reproducible results for the determination of LA, ML, DL, and TL in MCO samples.

Buccal administration of mucoadhesive blend films saturated with propranolol loaded nanoparticles.

The aims of this study were to prepare and characterize hydroxypropyl methylcellulose (HPMC)/polycarbophil (PC) mucoadhesive blend films saturated with propranolol hydrochloride (PNL)-loaded nanoparticles to improve permeability of drugs that undergo first-pass metabolism. An ionic cross-linking method and film casting technique was used to prepare nanoparticles and mucoadhesive blend films, respectively. Increasing concentrations of PNL (70, 80, 90 mg/film) in HPMC/PC blend films containing PNL-loaded nanoparticles (PN-films) and HPMC/PC blend films containing PNL (80 mg/film) without nanoparticles (PP-films) were prepared to test swelling, mucoadhesiveness, release, permeation and physicochemical properties. Scanning electron microscope (SEM) images showed a partially smooth surface with a wrinkled occurrence and spherically shaped, well-dispersed nanoparticles on the surface of PN-films containing PNL 80 mg/film (PN-films-80). The size of the nanoparticles on the surface of PN-films-80 was around 100 nm, which was similar to the nanoparticle size observed using light scattering technique. The swelling index (SI) of all PN-films and PP-films increased greatly in the first period time (10-20 min) and reached swelling equilibrium at 20 min and 30 min, respectively. For the PN-films, the concentration of PNL influenced the mucoadhesive properties and tended to be higher when the amount of PNL increased. Immediate release of all blend film formulations was found in early time points (10-30 min). After 120 min, the release of PN-films-70 was lower than the other PN-films. Permeation studies using porcine buccal mucosa showed that inclusion of nanoparticles in the films increased the permeability of PNL compared to PP-films. Therefore, buccal administration of mucoadhesive blend films containing PNL-loaded nanoparticles could be a promising approach for drugs that undergo first-pass metabolism.