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Reducing ulcerogenic effect of self-nano emulsifying drug delivery system of piroxicam Iis Wahyuningsih; Wahyu Widyaningsih; Silviana Wulandari
Pharmaciana Vol 8, No 2 (2018): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Piroxicam is antiinflammatory non-steroidal (AINS) drug group that has anti-inflammatory, analgesic and antipyretic effects. Like most other AINS drugs, piroxicam has low solubility and has gastrointestinal (ulcerogenic) side effects on long-term use. The nano-emulsifying drug delivery system (SNEDDS) is one of the technologies that can be used to overcome it. This study aims to determine the effect of ulcerogenic SNEDDS piroxicam compared with piroxicam formulas instead of SNEDDS. This study uses white rats male strain SD age 2-3 months and weight 100-200 grams of 40 rats. Rats divided into 5 groups. Group I was a normal control group, the test animals were given only water. Group II was a suspending control group treated with a 1% polyvinylpyrrolidone (PVP) solution, group III is a carrier control group treated with SNEDDS carrier which is a mixture of tween 80, virgin coconut oil (VCO) and polyethylene glycol (PEG) 400, group IV was a group of piroxicam drugs suspended with piroxicam 1.08 mg/kg in 1% PVP, group V was treated with SNEDDS piroxicam.Treatment was done for 28 days. After treatment, the gastric of rats were taken to be observed for ulcerogenic effects. Observations were made macroscopically by looking at ulcer scores followed by histopathological observations of tissue. The ulcer score data from each group were analyzed using one-way ANOVAand LSD test. The results showed that the normal control group, 1% PVP suspension and carrier group had a ulcer index of 0.0, 0.0 and 0.0, while the piroxicam suspension group and the SNEDDS group had an ulcer index of 0.88 and 0.0. These results were confirmed by histopathologic results of SNEDDS piroxicam to decrease the effect of pyroxicam ulcerogenic with results in the piroxicam suspension group has ulcer with necrosis by neutrophil infiltration, lymphocytes and mast cells in the mucosal tunica to submucosa. In the SNEDDS piroxicam group there is erosion with necrosis of the mucosal tunica epithelium with infiltration of lymphocytes and mast cells in submucosal tunica. It can be concluded the SNEDDS piroxicam can decrease the ulcerogenic effect.

BIOAVAILABILITAS TABLET IBUPROFEN PADA PEMBERIAN BERSAMAAN DENGAN EKSTRAK AIR HERBA PEGAGAN (Centella asiatica (L) Urban) PADA KELINCI JANTAN Depprelia Wahyu Sutanti; Iis Wahyuningsih
Pharmaciana Vol 3, No 1 (2013): Pharmaciana
Publisher : Universitas Ahmad Dahlan

The tendency to use herbal drug simultaneously with synthetic drug may result inan interaction. Based on research, aqueous extract of Centella asiatica (L) Urbancontains saponin (asiaticoside and madecassoside) compounds that inhibit CYP450and is a safe herbal alternative that is used for anti-inflammatory treatment. The aim ofthis study was to investigate the effect of aqueous extract of Centella asiatica (L) Urbanto the ibuprofen tablet bioavailability in male rabbits. Both compounds are metabolizedby CYP450 enzymes in the same way with different mechanism. The cross over designwith the same subject was used in this study. The samples consisted of 400 mg ibuprofenwith 0%b/v, 25%b/v, 50%b/v dan 100%b/v aqueous extract of Centella asiatica (L)Urban respectively. The blood were taken after 0; 0,5; 1; 1,5; 2; 2,5; 3; 3,5; 4; 6; 8; 10hours after samples treatment, then the ibuprofen plasma concentration weredetermined spectrophotometrically. The results then were used to evaluat thebioavailability parameters: tmaks, Cpmaks, and AUC and were analyzed using ANOVAtest in the same way as well as the 95% trust standart. The results showed, the use ofibuprofen tablet stimultaneously with aqueous extract of Centella asiatica (L) Urbanincreased Cpmaks dan AUC, but there were no influence to the tmaks value. The use ofibuprofen tablet stimultaneously with 50 %b/v and 100 %b/v aqueous extract ofCentella asiatica (L) Urban had a significant influence to the bioavailability ofibuprofen.

Nanoemulgel activity of Binahong (Anredera cordifolia (Ten.) Steenis) leaf extract againts wound healing of hyperglycemic rats Magfirah Septiani Yusuf; Iis Wahyuningsih; Sapto Yuliani
Pharmaciana Vol 13, No 1 (2023): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Hyperglycemia is associated with long-term damage, leading to the onset of wounds. The content of flavonoid compounds, steroids and saponins in Binahong leaves (Anredera cordifolia (Ten). Steenis) plays a role in the healing of diabetic wounds. The effectiveness of the active substance of the natural material is influenced by the large size of the particles, due to the presence of barier skin membranes. Nanoemulgel is an emulsion preparation with a droplet size of 1-100 nm which is suspended in a hydrogel. This study aims to determine the wound healing activity of diabetes in nanoemulgel preparations of binahong leaf extract (Anredera cordifolia (Ten.) Steenis) with its extract in male rats wistar hyperglycemia. The study was divided into 4 groups each consisting of 6 mice with diabetic wounds who got each a negative control group (glucose + nanoemulgel base), a positive control group (glucose + Madecassol 1%), a test group 1 (glucose + nanoemulgel, and a test group 2 (glucose + EDB). Treatment is carried out 2 times a day for 16 days. KGD measurements are carried out on the 0th, 1st, 5th, 14th and 21st days, and measurements of the diameter of the wounds are carried out on the 1st, 5th, 14th and 21st days. The KGD measurement results of the EDB nanoemulgel group decreased KGD by 52.91% on day 16 compared to the extract group which decreased by only 30.51% until the 16th day. The closure of the diabetic wounds of the EDB nanoemulgel group experienced closures of up to 52.91% compared to extracts that experienced closure of only 30.51% on day 16. The results of the one-way anova statistics showed a significant difference in the value of the decrease in kgd of the nanoemulgel preparation and its extract with the sig value. 0.045 and significant differences to the wound closure diameter of the diabetic EDB nanoemulgel group and its extract.

Development of transdermal patch preparations binahong leaf extract (Anredera cordifolia (Ten.) Steenis) and antihyperglycemia test in rats Galang Pergiawan Ramadhan; Iis Wahyuningsih; Wahyu Widyaningsih
Pharmaciana Vol 13, No 2 (2023): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v13i1.24602

Binahong leaves are plants that have great potential as antihyperglycemics, and have chemical content including triterpenoids, flavonoids, and saponins. However, the development of binahong leaves in pharmaceutical preparations is still very lacking. Objectives of this study are knowing the transdermal patch formulation of binahong leaf extract (BLE) produces good physical properties and the development of BLE transdermal patches with different extract concentrations may blood glucose lower (BGL) levels in glucose-induced mice. This study uses a single-layer patch because it has the advantage of being able to penetrate faster and is suitable for compounds that have solubility in polar solvents. The research began with the extraction of binahong leaves, then formulated a transdermal BLE patch using a formula that includes HPMC (polymer), glycerol (plasticizer), oleic acid (enhancer) and tween 80 (enhancer). Diabetic rats were divided into 4 groups of 6 rats, negative control group (glucose + placebo), positive control group (glucose + insulin), FI group (glucose+ transdermal patch BLE 30%), and FII group (glucose + transdermal patch BLE 47%). BGL measurements are carried out on the 0th, 3rd, 5th, and 7th days. The physical characterization carried out includes organoleptic, weight uniformity, thickness, pH, folding resistance, and moisture content, obtained FI and FII results that meet the requirements set out by each test standard. BGL (mg/dL) from day 1 to day 7 decreased in each group, positive control (68.8±3.76), negative control (112.5±6.89), FI (81.0±4.04), and FII (72.33±5.12). Based on the statistical results of the T-test on the physical evaluation of BLE transdermal patch preparations of FI and FII there were significant differences in weight and thickness uniformity, but there were no significant differences in pH, folding power, and humidity tests. The administration of a 47% BLE transdermal patch provides a faster but insignificant BGL reduction effect compared to the 30% BLE FI transdermal patch.

In-vivo study of oleic acid and tween-80 on patch transdermal A.paniculata as anti-diabetic Wahyuningsih, Iis; Fadilah, Nur Aini; Widyaningsih, Wahyu
Pharmaciana Vol. 14 No. 2 (2024): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v14i2.27851

Sambiloto (Andrographis paniculata) has been known empirically as a plant that has benefits as a traditional antidiabetic Javanese medicine to treat diabetes mellitus (DM). The main compound contained in sambiloto is andrographolide which has a hypoglycemia effect. Andrographolide has low solubility in water and poor bioavailability due to biotransformation by P-glycoprotein in the intestinal tract which causes andrographolide to metabolize more quickly in the duodenum and jejunum. To overcome this extract ethanol of sambiloto (EES) formulated to patch transdermal. Enhancers can affect the characteristics of transdermal patch preparations which affect the pharmacological activity of transdermal patch preparations. The critical point of transdermal patch preparation is the selection of enhancers which is one of the compounds to increase the penetration of active substances in the skin by disrupting the permeability of the stratum corneum. The aim of this research is to determine the effect of variations in the combination of oleic acid and tween 80 as an enhancer on the physical characteristics of EES patches.The methods of extraction sambiloto use soxhetation with ethanol 96% as solvent. The formulation of EES patch transdermal using solvent casting technique with various concentration enhancer tween-80 and oleic acid. This research was conducted by making 3 formulas, where F1 (1:1), F2 (1:3) and F3 (1:3). The evaluations include weight uniformity, thickness, water content, pH and folding endurance of the patch. The result of visual appearance the patch EES has a dark green with aroma specific of EES. The characteristics of EES transdermal patches were affected by the ratio of tween-80 and oleic acid as the enhancers. The combination of oleic acid and tween 80 as a permeation enhancer has an influence on physical characteristics (weight and thickness) of EES patches.

Reducing ulcerogenic effect of self-nano emulsifying drug delivery system of piroxicam Wahyuningsih, Iis; Widyaningsih, Wahyu; Wulandari, Silviana
Pharmaciana Vol. 8 No. 2 (2018): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v8i2.11478

Piroxicam is antiinflammatory non-steroidal (AINS) drug group that has anti-inflammatory, analgesic and antipyretic effects. Like most other AINS drugs, piroxicam has low solubility and has gastrointestinal (ulcerogenic) side effects on long-term use. The nano-emulsifying drug delivery system (SNEDDS) is one of the technologies that can be used to overcome it. This study aims to determine the effect of ulcerogenic SNEDDS piroxicam compared with piroxicam formulas instead of SNEDDS. This study uses white rats male strain SD age 2-3 months and weight 100-200 grams of 40 rats. Rats divided into 5 groups. Group I was a normal control group, the test animals were given only water. Group II was a suspending control group treated with a 1% polyvinylpyrrolidone (PVP) solution, group III is a carrier control group treated with SNEDDS carrier which is a mixture of tween 80, virgin coconut oil (VCO) and polyethylene glycol (PEG) 400, group IV was a group of piroxicam drugs suspended with piroxicam 1.08 mg/kg in 1% PVP, group V was treated with SNEDDS piroxicam.Treatment was done for 28 days. After treatment, the gastric of rats were taken to be observed for ulcerogenic effects. Observations were made macroscopically by looking at ulcer scores followed by histopathological observations of tissue. The ulcer score data from each group were analyzed using one-way ANOVAand LSD test. The results showed that the normal control group, 1% PVP suspension and carrier group had a ulcer index of 0.0, 0.0 and 0.0, while the piroxicam suspension group and the SNEDDS group had an ulcer index of 0.88 and 0.0. These results were confirmed by histopathologic results of SNEDDS piroxicam to decrease the effect of pyroxicam ulcerogenic with results in the piroxicam suspension group has ulcer with necrosis by neutrophil infiltration, lymphocytes and mast cells in the mucosal tunica to submucosa. In the SNEDDS piroxicam group there is erosion with necrosis of the mucosal tunica epithelium with infiltration of lymphocytes and mast cells in submucosal tunica. It can be concluded the SNEDDS piroxicam can decrease the ulcerogenic effect.

Application of vegetable oils as pharmaceutical ingredient: the impact of liquid lipid type on the characteristics of nanostructured lipid carrier Binarjo, Annas; Ernidawati; Khotimah, Khusnul; Wahyuningsih, Iis; Efiana, Nuri Ari
Pharmaciana Vol. 14 No. 3 (2024): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v14i3.30281

Recently, drug encapsulation using a Nanostructured Lipid Carrier (NLC) has gained attention in formulation studies due to its high loading capacity and prevent drug expulsion during storage. Drug loading capacity is mainly affected by lipid type and composition, especially liquid lipids. Therefore, this research aims to evaluate the potential of avocado oil as a liquid lipid of NLC replacing pure oleic acid. All components including oil, glyceryl monostearate, Tween 20®, and Span 60® were processed to NLC by solvent injection method. The colloidal characteristics of NLC dispersion in water and 20 mM PBS pH 7 were determined, including transmittance, particle size, size distribution, zeta potential, loading capacity (LC), and loading efficiency (LE) of capsanthin in NLC. The results showed that NLC containing oleic acid (Fola) and avocado oil (Favo) dispersion in PBS exhibited a similar transmittance and zeta potential of 69-74% and -51 to -58 mV, respectively, whereas the particle size and size distribution of Favo were significantly higher than Fola. Moreover, the 1.3-fold higher LC and LE of Favo compared to Fola was insignificant (p>0.05). Additionally, the Tween 20® and Span 60® ratio of Favo should be improved to obtain an ideal particle size and size distribution as in Fola. In conclusion, avocado oil indicated the potential to be utilized as a liquid lipid of NLC formulation regarding zeta potential and drug loading. However, the surfactant composition should be adjusted to reduce the particle size of the NLC, leading to permeability enhancement in delivery, particularly oral administration.

In-vivo study of oleic acid and tween-80 on patch transdermal A.paniculata as anti-diabetic Wahyuningsih, Iis; Fadilah, Nur Aini; Widyaningsih, Wahyu
Pharmaciana Vol. 14 No. 2 (2024): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v14i2.27851

Sambiloto (Andrographis paniculata) has been known empirically as a plant that has benefits as a traditional antidiabetic Javanese medicine to treat diabetes mellitus (DM). The main compound contained in sambiloto is andrographolide which has a hypoglycemia effect. Andrographolide has low solubility in water and poor bioavailability due to biotransformation by P-glycoprotein in the intestinal tract which causes andrographolide to metabolize more quickly in the duodenum and jejunum. To overcome this extract ethanol of sambiloto (EES) formulated to patch transdermal. Enhancers can affect the characteristics of transdermal patch preparations which affect the pharmacological activity of transdermal patch preparations. The critical point of transdermal patch preparation is the selection of enhancers which is one of the compounds to increase the penetration of active substances in the skin by disrupting the permeability of the stratum corneum. The aim of this research is to determine the effect of variations in the combination of oleic acid and tween 80 as an enhancer on the physical characteristics of EES patches.The methods of extraction sambiloto use soxhetation with ethanol 96% as solvent. The formulation of EES patch transdermal using solvent casting technique with various concentration enhancer tween-80 and oleic acid. This research was conducted by making 3 formulas, where F1 (1:1), F2 (1:3) and F3 (1:3). The evaluations include weight uniformity, thickness, water content, pH and folding endurance of the patch. The result of visual appearance the patch EES has a dark green with aroma specific of EES. The characteristics of EES transdermal patches were affected by the ratio of tween-80 and oleic acid as the enhancers. The combination of oleic acid and tween 80 as a permeation enhancer has an influence on physical characteristics (weight and thickness) of EES patches.

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