Sildenafil Citrate 2.5 mg/mL Oral Liquid

A spray-drying technique was utilised for solidifying liquid SNEDDS. It is crucial to convert liquid form into solid form, since liquid SNEDDS has several drawbacks.

Generally, liquid SNEDDS is encapsulated in soft gelatin capsules and these are susceptible to humidity.

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The thermal analysis was conducted via a differential scanning calorimetry (DSC Q200; TA Instruments, New Castle, DE, USA). Each sample (approximately 5 mg) was placed in standard aluminium pans and dry nitrogen was employed as the effluent gas. All samples were scanned at a temperature ramp speed of 10 sildenafil 45 mg chewable tablets °C/min and heat flow from 0 to 300 °C. X-ray powder scattering measurements were performed by means of an X-ray diffractometer (D/MAX-2500, Rigaku, Japan) at room temperature. An angular increment of 0.02° per second was selected over a range of 2θ angles from 3° to 50°.

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Dissolution profiles of sildenafil-loaded amorphous microspheres, crystalline microspheres, solid SNEDDS and the drug powder (equivalent to 10 mg of sildenafil) were investigated using Vision Classic 6 (Hanson Research Co.; Los Angeles, CA, USA). USP apparatus II (paddle method) was utilised. The dissolution medium was 900 mL of distilled water and the temperature was maintained at 37 ± 0.5 °C. The speed of the paddle was set to 50 rpm. At specific time intervals (0, 5, 10, 15, 30 and 45 min), an aliquot (3 mL) of the sample was collected, filtered through a 0.45 µm nylon syringe filter and assayed for the content of sildenafil by employing HPLC, as described above. In addition, incompatibility issues between gelatin shell and liquid SNEDDS might occur in the soft capsules.

For those reasons, there are many studies solidifying liquid SNEDDS using spray dryer.38,39 In this study, HDK N20 Pharma was chosen as a solid carrier, due to its porous surface and high BET value (175–225 m2/g).40,41 The sildenafil-loaded liquid SNEDDS was dispersed in water and HDK N20 Pharma was suspended. Consequently, the suspension was spray dried to manufacture sildenafil-loaded solid SNEDDS. To fabricate free-flowing powder, 500 mg of HDK N20 Pharma was required in order to absorb 1000 mg of liquid SNEDDS.

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Among the formulations with superior self-nanoemulsifying ability, emulsion droplet size of each drug delivery system was investigated (Figure 2B and C). As a result, the liquid SNEDDS composed of Labrasol, Transcutol HP and Captex 300 at a weight ratio of 70/15/15% was chosen, generating the smallest droplet size (150.3 ± 2.7 nm). The small-sized nanoemulsion has better solubilising capability than large-sized nanoemulsion, due to the increased surface area in contact with water. Additionally, nanoemulsion with fine droplet size possesses wide range of drug loading capacity and excellent biocompatibility. For this reason, SNEDDS with small droplet is usually preferred.36,37 Subsequently, sildenafil was loaded into the liquid SNEDDS. The surface morphological features were confirmed through a scanning electron microscope (SEM). Sildenafil exhibited irregular and oblong shape, assuming a crystalline solid form (Figure 3A). Amorphous microspheres appeared as small spherical particles clustered together (Figure 3B).

• It is not recommended for use in children or women.
• Overdose symptoms include dizziness, vision changes, and prolonged erections.
• Seek urgent medical help in case of overdose.

Compared to the drug powder, decreased particle size was observed in amorphous microspheres.

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Next, sildenafil was incorporated into the chosen liquid SNEDDS and highly porous inorganic materials with large specific surface areas (500 mg) were added for solidification. The suspension flowed through a pneumatic nozzle of 0.7 mm diameter in a Büchi mini spray dryer (B-290; Flawil, Switzerland) at a flow rate of 5.0 mL/min. The inlet temperature was set at 130 °C and the outlet temperature was maintained at 80 °C. The aspirator was set at 90% and the pressure of the spraying air was 4 kg/cm2. During the entire spray-drying process, the suspension was continuously stirred (500 rpm) using a magnetic bar to maintain a stable suspension state.

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The shape and surface of the samples were examined by employing an S-4800 scanning electron microscope (Hitachi; Tokyo, Japan). Double-sided adhesive tape was utilized to fix the samples. To render the sample electrically conductive, a platinum coating (4 min at 15 mA) was applied by utilising the EmiTeck Sputter Coater (K575 K) at a speed of 6 nm/min under vacuum (0.8 Pa). Particle-size analysis was carried out using Mastersizer 3000 (Malvern, Worcestershire, UK). The instrument was optimised under the following conditions: air pressure, 1 bar; feed rate, 50%; gab, 1. Nonetheless, the SEM image of the crystalline microspheres sildenafil spray indicated that the crystalline drug adhered to hydrophilic excipients, such as PVP and Labrasol (Figure 3C). Unlike the amorphous microspheres, the crystalline microspheres presented no significant particle size reduction, compared to the drug powder. However, the external region of the drug consisted of hydrophilic ingredients, which led to the production of an uneven surface in crystalline microspheres.

• Sildenafil oral solution is a liquid form of erectile dysfunction medication.
• It allows for easier swallowing compared to pills.
• Typically, it's used when oral tablets are unsuitable.

Furthermore, irregular spherules with smooth surfaces were scattered in the solid SNEDDS (Figure 3D).

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Then, the resultant suspension was spray dried while continuously stirring using a magnetic bar (500 rpm). The inlet temperature was maintained at 140 °C and the outlet temperature was set at 80–90 °C. The pneumatic nozzle, pump rate, aspirator value and spraying air pressure were consistent with the preparation conditions of the amorphous microspheres. The composition of liquid SNEDDS was selected on the basis of an aqueous solubility test. Afterwards, numerous ratios of oil, surfactant and co-surfactant were combined to create liquid SNEDDS formulations.

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The formulations containing various mixtures of oil, surfactant and co-surfactant were plotted in ternary-phase diagram (Figure S1). Furthermore, their dispersion in water was visually evaluated. Additionally, the nanoemulsion droplet size was assessed only for the formulations providing excellent nanoemulsifying ability (achieving the visual standard of the preceding experiment). The nanoemulsion droplet size was analysed via a Zetasizer Nano ZS (Malvern Instruments, Worcestershire, UK). Among the formulations, the liquid SNEDDS with the smallest emulsion droplet size was selected. HDK N20 Pharma is well reported to exhibit a highly porous surface and rough appearance.42,43 During the solidification process, oily liquid covered the porous surface of HDK N20 Pharma, resulting in the creation of a smooth surface. The particle-size distribution results are presented in Figure 4. The portions of particles with diameters below D50 are 50%. In general, the value of D50 indicates the median diameter. The drug powder gave an average size of 26.6 ± 0.9 µm.

In amorphous microspheres, a significant particle size reduction occurred (9.3 ± 1.0 µm), compared to sildenafil powder (p < 0.05). On the other hand, the crystalline microspheres exhibited a particle size of 27.8 ± 1.5 µm, similar to the particle size for the drug powder.

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Twenty-four rats were non-selectively divided into four groups (each group consisted of six rats). After the anaesthesia process, the femoral artery of the rats was inserted with a surgical tube and fixed on a surgical board. Before surgery, heparin (50 IU/mL) was prepared to coat the inside of the polyethylene tube. The sildenafil-loaded amorphous microspheres, crystalline microspheres, solid SNEDDS and the drug powder were placed in a #9 gelatin capsule and administered orally at a dose of 20 mg/kg. Plasma samples (300 µL) were collected at predetermined time points via the cannulated tube.

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After centrifuging the sample at 20,000 g for 10 min, the supernatant (100 µL) was separated. The protein precipitation method was applied while using revaprazan as an internal standard. Finally, the amount of sildenafil was analysed through HPLC. Statistically significant difference was confirmed by the Student’s t-test (for a pair of groups) and one-way ANOVA followed by Tukey’s post hoc test (for more than two groups). For the statistical calculation, SPSS sildenafil 25mg tablets Version 26 (IBM, Armonk, NY, USA) was utilised. The tendency of the particle-size analysis was consistent with the SEM results. The drug and ingredients were completely dissolved in ethanol and spray dried, leading to a decrease in particle size in the amorphous microspheres. In the preparation of crystalline microspheres, PVP and Labrasol were dissolved; however, hydrophobic sildenafil was undissolved in distilled water and the aqueous suspension was spray dried.

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A p-value of <0.05 was considered significant.33 Among the investigated ingredients, PVP and Labrasol were selected as a proper polymer and surfactant, respectively, due to their high solubility as shown in Figure S2-A and B. Afterwards, various amorphous microspheres were prepared (Table S1). To determine the optimal weight ratio of the drug, PVP and Labrasol, aqueous solubility and dissolution test were carried out as shown in Figure S3-A and B. As a result, the optimised amorphous microspheres were composed of PVP/ Labrasol/drug at the weight ratio of 6/1/1, showing the highest solubility and dissolution rate (%). The same configuration selected in the amorphous microspheres was utilised in the crystalline microspheres; however, this drug delivery system was produced using distilled water instead of an organic solvent.

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The final compositions of amorphous and crystalline microspheres are presented in Table 1. In this study, ingredients that maximise drug solubility were selected as components of SNEDDS, according to the previously published studies.20,31 The drug showed the highest solubility in Captex 300 among the oil stocks (Figure S4). Furthermore, Labrasol and Transcutol significantly increased the solubility of the drug, compared to others. Therefore, Captex 300, Labrasol and Transcutol were selected. The appropriate ratio of Captex 300, Labrasol and Transcutol was determined by the nanoemulsion-inducing ability and nanoemulsion droplet size, established in the previous methods.34,35 In the absence of sildenafil, the nanoemulsifying capability of liquid SNEDDS in water was evaluated along with visual standards as shown in Figure 2A.