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Background: Diclofenac potassium is an NSAID drug that is used in the treatment of mild to moderate pain. The use of this drug orally can cause side effects in the gastrointestinal tract, and the drug will undergo extensive first-pass metabolism in the liver. Therefore, preparations for transdermal patches were made. Objective: Determining the effect of the polymer ratios of carboxymethyl chitosan, polyvinyl pyrolidone K-30, and ethyl cellulose N22 on the physicochemical characteristics and drug release of a matrix type diclofenac potassium patch. Methods: In this study, matrix type diclofenac potassium patches were made using a combination of carboxymethyl chitosan (CMC), polyvinyl pyrrolidone (PVP) K-30 polymer, and ethyl cellulose (EC) N22 in a ratio of 2:3:7 and 3:2:7. Patches are made by mixing the entire polymer matrix and diclofenac potassium together, which are then evaporated and dried. Results: The results showed that the different polymer compositions of CMC, PVP K-30, and EC N22 resulted in patches with physicochemical characteristics that were not significantly different. The combination of these polymers is able to control the release of the drug from the patch for a long time. It was also found that increasing the concentration of CMC was able to increase the rate of release of diclofenac potassium. Formula 2 with a ratio of 3:2:7 is claimed to be the best formula in terms of physical, chemical, and drug release characteristics from the patch. Further studies are needed, such as drug penetration tests into the skin.

Background: Skin aging can be overcome by applying anti-aging cosmetics. Many active ingredients that have anti-aging potential are derived from plants, and these materials must be delivered with a sound skin delivery system, namely nanoemulsion. The characteristics of nanoemulsion are closely related to physical stability. Objective: This study aims to conduct a systematic review of in vivo and in vitro study designs to examine the characteristics and physical stability of nanoemulsions used in topical anti-aging cosmetics. Methods: A systematic literature review based on the PRISMA statement was used to review the articles regarding nanoemulsions’ characteristics and physical stability. The article search was accessed from an internet search database: Scopus, Pubmed, and Web of Science, published between January 2012 and June 2022. Results: Of the 244 articles, 44 were found to be related to the characteristics and physical stability of nanoemulsions in anti-aging cosmetics. These showed that active ingredients with antioxidant activity, filter UV rays, moisturizing agents, and cell-repairing agents are delivered by a nanoemulsion system with various types and ratios of surfactants, cosurfactants, and oil phases. Tween 80, Span 80, Transcutol HP, and Caprylic/capric triglyceride are the most widely used nanoemulsion compositions. Conclusion: The type and composition of the oil phase, surfactant, and cosurfactant affect the characteristics of the nanoemulsion (droplet size, polydispersity index, viscosity, zeta potential) and the physical stability of the nanoemulsion so that it can deliver active ingredients that have the potential as anti-aging well.

Inhalation Ciprofloxacin HCl microspheres were formulated with combination of alginate and kappa carrageenan with a total of 1% (F1), 1.5% (F2), and 2% (F3). Aim of this research is to examine effect of polymer concentration on characteristics, release, and lung deposition of microspheres. Microspheres were characterized including loading, efficiency, yield, size, moisture content, mucoadhesivity, and release. Deposition was studied by fluorescence microscopy. Results showed spherical and smooth with size ofless than 2 µm. Loading showed about 18.55% to 29.65%. Entrapment efficiency was 52.86-76.29%. Yield was 49.83-70.72%. Swelling index was less than 10. For moisture content, all formulas demonstrated less than 6.5%. For mucoadhesivity, F1, F2, and F3 showed 0.0090 kg, 0.0217 kg, and 0.0329 kg respectively. It was found that increasing polymer concentration did not affect size, loading, efficiency, and yield of microspheres. Cumulative release at F1, F2, and F3 was 72.64%, 59.25%, and 47.66% respectively in 10 minutes at PBS pH 7.4 with burst release profile. In vivo showed that all formulas were able to deposit on rat lungs and it was found that the intensity were decreased at the 4th hour due to increase of polymer. Remaining intensity indicated that microspheres were able to maintain the drugs loaded.

The aim of this study was to determine the effect of different concentration of carboxymethyl chitosan and curcumin on physical characteristics and wound healing activity of carboxymethyl chitosan-curcumin hydrogel. Hydrogels were prepared using carbomer as a gelling agent and TEA was added to neutralize the carbomer hydrogel in order to make it swell. The obtained hydrogels were evaluated for its physical characterization such as organoleptic, viscosity, spreadability, drying time, pH, and wound healing activity on the burned wound in Wistar rats. The results showed that higher concentration of carboxymethyl chitosan significantly reduces viscosity and pH while its spreadability and drying time are significantly increased. Curcumin only affected two out of five physical characteristics: organoleptic and pH. Higher concentration of curcumin reduces its pH but statistical analysis showed no interaction between carboxymethyl chitosan and curcumin. The wound healing activity in Wistar rats with 2nd degree burn wound model indicates that carboxymethyl chitosan-curcumin hydrogel can significantly improve wound healing activity in rats compared to control group. Higher concentration of carboxymethyl chitosan can affect the physical characteristics of carboxymethyl chitosan-curcumin hydrogel i.e. a decrease in viscosity and pH, as well as an increase in spreadability and drying time. On the other hand, higher concentration of curcumin only affected the pH of the preparation. In the wound healing activity test, macroscopic observation showed that the combination of carboxymethyl chitosan-curcumin significantly increased the wound healing activity of 2nd degree burn in Wistar rats. However, the use of this hydrogel preparation statistically did not give significant improvement in wound healing process when compared with G1, G2, G3, G4, and positive control. Based on histopathology test results, it can be concluded that after 14 days of treatment the value of collagen deposition and PMN between groups 1, 2, 3, 4, and positive control and intergroup replication (1, 2, 3, 4, and positive controls) are in uniformity which indicates that the wound has undergone healing process. In addition, the four groups possess better results than negative controls which didn’t receive any treatment.

Gentamicin sulfate is a broad-spectrum aminoglycoside antibiotic that can be used for primary and secondary infections of the skin. Microspheres can be used to extend drug release on the skin; the resulting therapeutic effect is constant and has a longer duration of action. Therefore it can reduce the frequency of use and increase patient compliance. This study investigated the appropriate profile and release kinetics model of gentamicin sulfate microspheres entrapped on the emulgel base. Gentamicin-alginate microspheres were made by the ionotropic gelation method with aerosolization technique, using 2.5% Na-alginate low viscosity, CaCl2 solution of 1.5M as a crosslinker, maltodextrin as lyoprotectant and were dried using the freeze-drying method. The result of microspheres characterization, gentamicin microsphere was spherical with smooth surface structure and had particle diameter of 3.021 ± 0.017μm. Gentamicin microspheres had moisture content 2.89%, and maximum swelling index was 2625 ± 21.70% was achieved within 5 hours. The drug loading of microspheres was 1.75 ± 0.11%, and entrapment efficiency was 10.96 ± 0.19%. The release evaluation during 720 minutes showed that the amount of gentamicin release from alginate microspheres on emulgel base was 14.857 ± 0.816%, and gentamicin release on emulgel conventional was 49.239 ± 5.954%. The model of release kinetics of gentamicin microspheres on emulgel was Higuchi model that showed the release of the active ingredient through the diffusion process. While the model of release kinetics of gentamicin on emulgel base was first order, that showed the release of active agent depends on remaining concentration.

This study aims to determine the effect of the combination of beeswax and oleum cacao on the characteristics and stability of nanostructured lipid carrier-aleurites moluccana seed oil (NLC-AMs oil). The combination ratio of beeswax-oleum cacao and AMs oil is 3:1 which total lipid 20%, while the ratio of beeswax-oleum cacao used were F1(100:0); F2 (50:50); F3 (25:75); and F4 (0:100). These preparations are made by the high shear homogenization method because the processing technique is relatively easier, faster and it is possible to get nanoparticle size. Then characterization and physical stability test (real time, thermal cycling test, and centrifugation) were carried out. The results of this study can be concluded that: 1) NLC-AMs oil with combinations of beeswax and oleum cacao has smaller particle size than those using only single solid lipids (oleum cacao or beeswax). 2) Increased concentration of oleum cacao in the NLC-AMs oil system increases its viscosity. 3) The ratio of beeswax and oleum cacao affects the recrystallization index of the NLC-AMs oil. The lowest recrystallization index is in the NLC-AMs oil with a combination of beeswax-oleum cacao in F2 (50:50). 4) The results of the real time stability test for 8 weeks of storage revealed the NLC-AMs oil system with a combination of solid fat beeswax and oleum cacao on F3 (25:75) had the best stability. 5) All formulas are not stable against extreme temperature changes (thermal cycling test) and shocks (centrifugation) indicated by system separation.

Ubiquinone (co-Q10) is a topical anti-aging with low solubility in water, so its penetration into the skin is also low. To increase its penetration ubiquinone (co-Q10) was loaded in the nanoemulsion delivery system using virgin coconut oil (VCO) as oil phase. Ubiquinone (co-Q10) in nanoemulsion formula consists of; ubiquinone (co-Q10), Tween 80, Span 80, ethanol 96%, VCO and acetate buffer solution pH 4.2 ± 0.5 with concentration; 1%; 18.66%; 1.92%; 3.42%; up to 100%, respectively. The characteristics of ubiquinone (co-Q10) nanoemulsion were observed in terms of droplet morphology by transmission electron microscope (TEM) and droplet size by particle analyzer, the pH and viscosity value. The ubiquinone (co-Q10) penetration test in the nanoemulsion system was compared with the emulsion on the rat skin. Result of this research showed the droplet morphology of ubiquinone (co-Q10) in nanoemulsion was spherical. The droplet size was 93.2 ± 2.78 nm. The pH value was 4.12 ± 0.02, and the viscosity was 8.5 cPas. Penetrasi of ubiquinone (co-Q10) in nanoemulsion was deeper (269 ± 48.12 and 993 ± 36.49 μm) than in emulsion (26.33 ± 6.43 and 110.33 ± 9.124 μm), after 2 and 6 hours sample application.

The aim of this study was to investigate the ability of NLC in increasing photostability of tomato extract in term of antioxidant activity. Photostability testing on antioxidant activity of samples were conducted by accelerating method using UVB radiation 32.400 joule for 21 hours radiation. Antioxidant activity was measured by DPPH method. NLC was made by High Shear Homogenization (HPH) method at 24000 rpm for 4 cycles, while conventional creame was made by low speed at 400 rpm. The product were characterized include: pH, viscosity, and particle size. There were had difference characters and physical stability. NLC had smaller size, more homogenous and more stable than conventional creame. It was known that stability of antioxidant activity of tomato extract in NLC system higher than in conventional creame. That was showed with k value, as constanta of rate scavenging activity decreasing in antioxidant power between time (Sigma 2-tail less than 0.005) of NLC and conventional creame were: 2.03x10-2 %/hour ±0.08 (3.94) and 4.71x 10-2 %/ hour ±0.23 (4.88) respectively.

Ubiquinon (Q10) is an endogenous antioxidant. It is lipophilic and practically insoluble in water. To improve its solubility and penetration, it was formulated into O/W nanoemulsion. The resulting Q10 nanoemulsion was then physically characterized for its droplet size, morphology, and viscosity. In addition, it was conducted a penetration test of Q10 in nanoemulsion delivery system compared to Q10 in emulsion using male Wistar rats. From the characterization results, it was found that the droplet size of Q10 nanoemulsion (70.07 ± 12.42 nm) less than Q10 emulsion (21.063 ± 3,57μm), the morphology of droplet Q10 nanoemulsion and Q10 emulsion that are spherical, and that the viscosity of Q10 nanoemulsion (10.5 CPa.s) less than Q10 emulsion (16 CPa.s). The penetration rate of Q10 in nanoemulsion and emulsion was observed at 2 hours, 4 hours, and 6 hours after treatment. The result was known that the penetration rate of Q10 in nanoemulsion (174.49 μm/h) > Q10 in emulsion (20.429 μm/h).

Penetration is an absolute requirement for active ingredient to produce an effect in deep of the skin. First obstacle for active ingredient to penetrate through the skin is stratum corneum. Nanotechnology that has nano size particles, is the answer to make it’s penetrate through the skin. In this research the skin penetration of Coenzyme Q10 was loaded in the lipid nanoparticles that is nanostructure lipid carrier (NLC) was compered with it was dissolved in olive oil. The research result known that Coenzyme Q10 was loaded in NLC has deeper penetration (639.34 ± 17.69 µm) in the mice skin than it was dissolved in olive oil as control (33.00 ± 1.71 µm), its just least penetrated into the skin after 6 hours sample application.

Purpose: To investigate the effect of drug and polymer ratio on the physical characteristics and release rate of metformin hydrochloride from alginate microspheres.Methods: Microspheres were prepared by ionotropic gelation aerosolization technique using sodium alginate as polymer and calcium chloride as crosslinker. Three formulations of drug and alginate polymer ratios: 1:1 (F1); 1:1.5 (F2); and 1:2 (F3), and 10 % calcium chloride (CaCl2) were investigated. The microspheres were studied with respect to physical characteristics, release profile and release rate. Release evaluation was done at pH 1.2 in hydrochloric acid (HCl) for 2 h, and in phosphate-buffered saline (PBS) at pH 7.4 for 12 h.Results: Drug loading in formulations F1, F2 and F3 were 3.08 ± 0.21, 3.34 ± 0.28, and 3.99 ± 0.19 %, respectively. Low entrapment of below 15 % was achieved for all formulations, whereas high yield (above 45 %) was obtained. Drug release above 74 % was observed for all formulations. The release rates of F1, F2 and F3 were 9.6390 x 10-2, 9.0985 x 10-2, and 8.3312 x 10-2 %/min, respectively.Conclusion: Metformin-alginate microspheres can be used for optimized formulations with good physical characteristics and in vitro release. These findings suggest that the microspheres might be a potent drug delivery system for the treatment of diabetic mellitus.Keywords: Metformin, Alginate microspheres, Drug-polymer ratio, Aerosolization, Drug release