Combination Of HPMC Research Articles

Controlled Release Lercanidipine Tablets: A Study on Formulation and Evaluation by Wet Granulation

Lercanidipine blocks the entry of extracellular calcium into vascular and cardiac muscle cells, preventing myocardial smooth muscle contraction due to decreased intracellular calcium. This results in the dilation of coronary and systemic arteries, reducing blood pressure. This study aimed to develop and evaluate lercanidipine controlled-release tablets for oral administration using polymers like HPMC K 100M, sodium alginate, and guar gum. Lercanidipine, polymers, and diluents were sieved and mixed for 10 minutes. Granules were formed using isopropyl alcohol, dried at 60°C for one hour, and sieved. The granules were lubricated with colloidal silicon dioxide (Aerosil-200) and magnesium stearate, blended for 5 minutes, and compressed using a rotary machine (average weight: 500 mg; hardness: 5-6 kg/cm²). Bulk and tapped densities were nearly identical for all formulations. Compressibility index and Hausner ratio ranged from ?18 to 1.09-1.21, indicating good flow properties. Tablet thickness ranged from 5.82 to 5.91 mm, hardness from 5.9 to 6.3 kg/cm², and friability was less than 1.0 %W/W. Drug content was between 98-102%. The controlled-release order from dissolution data was F9 > F7 > F8, showing optimal release with a combination of HPMC and two natural polymers.

Formulation and evaluation of transdermal patch of carbamazepine

Transdermal drug delivery system (TDDS) is a widely accepted mode of drug delivery method due to various advantages and one of the novel routes for systemic delivery of drugs through intact skin. Topical drug administration is a systemic and localized method of delivering drugs through skin and is considered an attractive alternative to oral and parenteral routes. The aim of present study was to formulate and evaluate Matrix type transdermal drug delivery system (TDDS) of Carbamazepine was prepared by the solvent evaporation technique. Several batches were prepared by using combination of HPMC E-15, Eudragit RL-100, and Ethyl Cellulose different ratios. Propylene glycol was used as plasticizer and DMSO was incorporated as a permeation enhancer. These Formulated transdermal patches were characterized for their physicochemical parameters like thickness, weight variation, folding endurance, percentage moisture uptake, Percentage moisture uptake and In vitro drug release studies were examined. Among the above all formulation F6 was chosen as a best Formulation, because this optimised formulation showed satisfactory drug content, physical characteristic for its thickness, weight uniformity, percentage moisture content, percentage moisture uptake, and maximum % of drug release i.e., 93.95 % in 12 hours. The optimized formulation (F6) showed maximum highest percentage of drug release.

FORMULATION OF PEEL-OFF GEL MASK OF COCOA SKIN EXTRACT (Theobroma cacao L) WITH VARIED CONCENTRATION GELLING AGENT

Cocoa shells are waste from the plantation industry, with a fairly good potential source of energy and protein. The ethanol extract of cocoa shells contains alkaloids, flavonoids, phenols, and tannins. Cocoa shell extract has strong antioxidant activity with an IC50 value of 17.21 ppm and has sunscreen activity. This study aimed to determine the formulation and physical test of a peel-off gel mask with cocoa shell extract (Theobroma cacao L) and to determine its effect. The research method used was an experimental method with variations in the concentration of a combination of HPMC and PVA of 2%:10%, 3%:9%, 4%:8%, 5%:7%, and 0%:12%. The physical tests used on the peel-off gel mask with cocoa shell extract (Theobroma cacao L) included organoleptic, homogeneity, pH, spreadability, drying time, adhesiveness, viscosity, and cycling tests. Based on the results of the research carried out, peel-off gel mask has the characteristics of a brown color, a distinctive extract smell and a thick texture, homogeneous for F1 and F5, and not homogeneous for F2, F3, and F4, sticking force 4.53±0.24 seconds; 5.45±0.36 seconds; 8.94±0.64 seconds; 11.23±0.72 seconds; 3.87±0.70 seconds; spreadability 3.99 ± 0.18 cm; 3.33±0.31 cm; 3.47±0.78 cm; 3.32±0.50 cm; 3.05±0.42 cm; pH 6.17 ± 0.10; 6.16±0.03; 6.15±0.10; 6.11±0.05; 6.42±0.03; viscosity 19481.10±201.10; 20165.50±1.05; 20165.73±2.02; 20182.53±9.47; 14618.40±158.48. The physical stability of the gel mask preparations after treatment showed that the results of the peel-off gel mask preparations, F1 and F5, were stable. Keywords: peel-off gel mask, cocoa shell, extract, gelling agent

Formulation and evaluation of floating tablet of nimesulide by direct compression method

Nimesulide has been used versatile on fever, pain, inflammation, rheumatoid arthritis, tendinitis, thrombophlebitis and trauma. Common drawbacks of conventional tablet dosage forms of nimesulide show an irritant effect on the stomach due to its weakly acidic nature along it has short duration of action leading to poor bioavailability. A Floating drug delivery system for Nimesulide leads to overcoming the problem related to an irritant on the stomach by avoiding direct contact with the mucosa. Thus, this study was designed and performed to formulate and evaluate the floating tablet of Nimesulide and determine the release pattern of the prepared formulation. Tablets were prepared by direct compression method using different polymers (HPMC, carbopol, and guar gum), either in an individual or in combination. The formulation blend was subjected to various pre-formulation and post-formulation studies including floating lag time, total floating time, hardness, friability, drug content, weight uniformity, and in-vitro dissolution. According to pre- pre-formulation study, the flow property was found to be good to passable. Similarly, all post-compression parameters of floating tablets were found to be within acceptable limits except the friability test of F1 and F2 formulations. The tablet’s floating lag time was determined to be in the range of 7-153.5 seconds, and the total floating time was in the range of 4-7 hrs. From the data of dissolution, carbopol showed a slower release of drugs than that of HPMC and guar gum. The use of carbopol as a floating polymer showed release of drugs from dosage form was 84.46% in 7 hrs and 99.10% in 3 hrs with the use of HPMC, 96.39% in 4 hrs with the use of guar gum. A combination of HPMC and guar gum released drugs in a slow release of drugs only for 3 hrs i.e. 98.02% in 3 hrs, the combination of carbopol and HPMC slowly released drugs for 6 hrs i.e. 90.43% in 6 hrs, and the combination of carbopol and guar gum showed maximum slow release of drugs for greater than 7 hrs i.e.74.16% in 7hrs. Hence, among all the formulations, F7 with the combination of carbopol and guar gum as polymer showed a maximum slowed release effect for greater than 7 hrs, which can be taken as the best batch.

ANTI-ACNE PATCH FORMULATION SILKWORM COCOON WASTE WITH HPMC AND PVP VARIATIONS

Some topical preparations for acne have been developed in the form of gels and creams. However,it is still rarely developed in the form of a patch dosage form. Waste from silkworm cocoons has theactivity of inhibiting the growth of acne-causing bacteria, can be formulated into patch preparations.This study aims to formulate anti-acne patches from silkworm cocoon waste with variations of HPMCand PVP. The formulation of the anti-acne patch from silkworm cocoon waste was made by mixingthe lyophilisate of silkworm cocoon waste with a patch base with variations of HPMC and PVP. Theformulations were divided into 3 with different concentrations of HPMC and PVP additives, namelyformulas 1 (4:1), 2 (2,3:1), and 3 (1:1), respectively, The evaluations carried out included organolepticexamination, patch thickness, weight uniformity, fold resistance, moisture absorption, drying shrinkage.The results obtained showed that the concentration of the combination of HPMC and PVP polymersin the patch preparation gave different results from all evaluations that had been carried out, includingorganoleptic evaluation, weight uniformity, fold resistance, and drying shrinkage were in accordancewith the requirements of a good patch. The optimum concentration of the combination of HPMC andPVP as a polymer in the anti-acne patch preparation from silkworm cocoons is formula 2 with a ratioof (2,3:1) as novelty in this study.

The Effect of Variations in HPMC and Carbopol Bases on The Physical Stability of Okra (Abelmoschus esculentus L.) Fruit Gel Formulations

Okra fruit (Abelmoschus esculentus L.) is a vegetable that is often used as medicine. Okra fruit contains flavonoids which are antioxidants. Gel formulation with a concentration of 5%, and various combinations of HPMC and carbopol bases. This research aims to determine the physical stability of gel preparations and the effect of variations in the concentration of gelling ingredients in the preparations. The gel formulation consists of 4 formulas, namely F0, F1, F2, and F3. Physical stability tests include organoleptic tests (odor, color and texture), homogeneity, pH, spreadability, stickiness, viscosity and synergy. Tests were carried out for 14 days of storage, namely on days 1, 3, 5, 7, and 14 at room temperature (25℃). The observation results showed that in the organoleptic test there was no change in color, odor and texture in the gel preparation during 14 days of storage. The four gel formulas are homogeneous and there is no synergy. Variations in the combination of HPMC and carbopol bases affect the physical properties of the gel, including pH, viscosity, spreadability and adhesion. HPMC and Carbopol affect the pH of the preparation, the higher the Carbopol content and the lower the HPMC content, the more acidic it is. Carbopol and HPMC affect the values of spreadability, viscosity and adhesion because the higher the concentration of carbopol and HPMC produces a thick gel preparation so that the spreadability decreases, viscosity increases and adhesion also increases.

PHARMACOKINETIC STUDY IN HUMANS AND IN VITRO EVALUATION OF BIOENHANCED BILAYER SUBLINGUAL FILMS FOR THE MANAGEMENT OF ACUTE MIGRAINE

Objective: Long-lasting migraine pain is one of the most disabling neurological disorders and requires a quick onset of action from the administered dosage form. This study aimed to provide sublingual administration of the frequently used combination of NSAID and triptan in order to trigger their action immediately by escaping the first-pass metabolism, simultaneously improving patient compliance. Methods: In the present research, sublingual bilayer films were developed by joining the two loaded layers with zolmitriptan and piroxicam, respectively. Each layer was prepared and loaded separately using the traditional solvent casting method. Mechanical support was provided by the 1:1 combination of HPMC E-15 and pullulan, which were used as water-soluble film-forming polymers with polyethylene glycol 400 as a plasticizer. Films were evaluated for various physicochemical and mechanical properties. Finally, a pharmacokinetic study was performed on six healthy human volunteers to compare the PK parameters of the best formulation, BSTF-3, with those of a commercially available formulation. Sepitrap 80 and Sepitrap 4000 were used as bio-enhancers to achieve faster systemic delivery. Results: The thin, flexible bilayer films were observed to provide quick action alone with increase patient compliance by preventing the first-pass metabolism and dysphagia. Sepitrap 80 successfully increased the permeation of both drugs. Approximately 92 percent of zolmitriptan was released from the formed bilayer sublingual thin films within 3 min, whereas 92 percent of piroxicam was released within 4.5 min from the best formulation. Within 30 min of the commencement of the pharmacokinetic investigation, plasma concentrations of the active component began to rise rapidly. Conclusion: When compared to commercial formulations, the developed films had a greater AUC and Cmax with a shorter Tmax, indicating a faster trigger of action and higher bioavailability.

Preparasi dan Karakteristik Floating Tablet Ekstrak Daun Jambu Biji (Psidium guajava L.) dengan Variasi Kombinasi Xanthan Gum dan HPMC

Floating drug delivery system (FRDDS) is a new drug delivery system that is intended to prolong the time of drugs in the stomach. One form of the gastroretentive system is a floating tablet, which can float and stay in the stomach for some time. Preparations with this system are suitable for use in drugs that have an action on the stomach. Gastritis is defined as an inflammation or swelling of the inner lining of the stomach. Guava leaves are proven to have active ingredients that can act as anti-ulcers. This study aims to formulate floating tablets and determine the optimal combination of HPMC with xanthan gum in the formulation of floating tablets of guava leaf extract based on flotation testing and in vitro dissolution profiles. The extract was made using maceration method with 96% ethanol as solvent. The tablets were made in a number of 3 formulas using the wet granulation method. Each tablet weighed 500 mg with a combination of various types of HPMC K100M, HPMC K15M, HPMC K4M with xanthan gum as a floating agent. The formula produced the best tablet quality with a combination of HPMC K100M and xanthan gum as a floating agent. Based on the results of the in vitro dissolution profile, the drug release rate ranged from 23,604% - 26,846% with in 360 minutes (6 hours).

DEVELOPMENT AND CHARACTERIZATION OF SUSTAINED RELEASE GASTRO-RETENTIVE FLOATING TABLETS OF AMBROXOL HYDROCHLORIDE

Introduction: The objective of this study was to formulate floating tablets of Ambroxyl hydrochloride (AMB HCl) using the dry granulation technique to increase its bioavailability and the gastric residence time (GRT) of the dosage form. Materials and Methods: The gastro-retentive floating tablets of Ambroxol hydrochloride (AMB HCl) were prepared by direct compression method using different concentrations of polymers such as HPMC K4, HPMC K15 and PVP K30, gas releasing agents (Sodium bicarbonate and citric acid) and diluents (Microcrystalline cellulose). Citric acid was also used as an antioxidant. The final mixing was done by adding talc and magnesium stearate to the granules. Results and Discussion: The prepared formulation of AMB HCl was evaluated by some evaluation parameters such as hardness, friability, weight variation, buoyancy lag time, drug contents, total floating time, in vitro dissolution study, drug release study etc. The result from the FT-IR data study of formulation it was disclosed that there is no interaction between the drug and excipients. In the FT-IR study, it was revealed that there is no interaction between the drug and excipients. The formulation containing the combination of HPMC K 15M polymer and Sodium bicarbonate shows a good drug release pattern with less floating lag time and good floating duration. In vitro drug release study of the prepared formulation (gastro retentive floating tablets of AMB HCl) was shown that the formulation F5 was the best formulation which was found to be 99.87% drug release. The release mechanism and its kinetics were evaluated by plotting various mathematical models of release data such as the Higuchi model, Korsmeyer model, First order and Zero order drug release. The optimized formulation showed no significant change at various evaluation parameters such as hardness, friability, weight variation and % drug release for accelerated stability condition at 40±2oC temperature and 75±5% (RH) relative humidity for 3 months. The floating tablets of AMB HCl showed their potential over a prolonged period as a gastro retentive drug delivery system (GRDDS).

APPLICATION D-OPTIMAL METHOD ON THE OPTIMIZATION OF FORMULATION OF KINTAMANI ARABICA COFFEE GEL (Coffea arabica L.)

Arabica coffee (Coffea arabica L.) kintamani is a superior agricultural product from Bali. Arabica coffee (Coffea arabica L.) contains many compounds, one of which is caffeine which is beneficial for health and beauty. This study aims to formulate kintamani arabica coffee beans into a gel dosage form. The optimization formula of kintamani arabica coffee bean gel was made using the D-Optimal method using a combination of HPMC and propylene glycol as observation variables and spreadability, pH, and viscosity of the gel preparation as experimental responses. The study of caffeine from the gel preparation was carried out using a Franz diffusion cell. Caffeine content in the gel preparation and its release are determined by spectrophotometric method. The results showed that the amount of HPMC used would increase the viscosity value (+14113.92) and decrease the spreadability (-0.29) and pH (-6.59167E-003) of the gel. The greater the amount of propylene glycol used will decrease the viscosity value (-2484.54) and increase the spreadability value (+0.30) and pH (+0.31802) of the gel. The conclusion of this study is the use of a combination of HPMC and propylene glycol (6%:17%) resulted in the optimum formula with a viscosity value of 44,070 cps, a spreadability value of 3.6 cm, and a pH value of 5.32. The caffeine content obtained in the gel preparation was 188.47 g and the amount of caffeine released from the gel preparation for 6 hours of testing was 4.95%.

Research the influence of excipients on the technological properties of captopril fast dissolving films

Drug-loaded films are of great interest among fast-dissolving drug-delivery systems. The creation of fast-dissolving films for the treatment of cardiovascular diseases is important.The first inhibitor of angiotensin-converting enzyme to appear on the world market was captopril, which is used to treat hypertension, chronic heart failure and others. Captopril has an antihypertensive effect, which manifests itself within 5–15 minutes after sublingual administration.
 The aim of our study was to develop the technology of captopril fast dissolving films by solvent casting method and analyze the influence of groups of excipients on technological properties of the films.
 The influence of the character of polymers, plasticizers, disintegrants and sweeteners on the technological properties of experimental batches of captopril fast dissolving films was studied. Such technological indicators as uniformity of weight, thickness, swelling index,tensile strength, elongationand disintegration time were studied.
 The influence of excipients' composition on the technological indicators of captopril fast dissolving films has been researched. It was found out that the effect of the type of polymer had the decisive influence on all parameters of films.The selected plasticizer determined the elasticity (films' elongation), film thickness and weight variation. Optimal values of the average weight and thickness of captopril films are provided by the use of a polymer in the combination of HPMC with PEG 4000 or a combination of HPMC with PEG 6000, as a plasticizer – glycerin or PEG 400. The best results of films' swelling were obtained with the introduction of HPMC brands Metolose® 90 SH 100 000 or Metolose® 65 SH 50, Polyplasdone XL-10 crospovidone, propylene glycol and sorbitol. The disintegration time less than 3 min was observed in all investigated film compositions, except those containing PVA. The highest value of tensile strength for captopril films was obtained using HPMC brand Metolose® 65 SH 50 or Metolose®90 SH 100 000.
 Using the desirability function, the optimal excipients within the studied groups were selected.It has been established that the optimal values of the technological parameters of captopril films can be achieved using Hydroxypropyl MethylcelluloseVivapharm® E15, polyethylene glycol 400, sodium starch glycolate and sorbitol.

Pengaruh Konsentrasi HPMC-Kitosan terhadap Sifat Fisik dan Aktivitas Antioksidan Serum Ekstrak Pegagan (Centella asiatica L. Urban)

The use of pegagan (Centella asiatica L.) is an important spotlight in the development of pharmaceutical dosage forms, especially in the scope of cosmetic preparations. Pegagan (Centella asiatica L.) contains secondary metabolites such as flavonoids, phenolics, saponins, and steroids which are natural antioxidants from a plant. This study aims to be able to apply the benefits of pegagan (Centella asiatica L.) in the manufacture of pharmaceutical preparations in the form of facial serum made in three concentrations of HPMC as a gelling agent, namely 4%, 6%, and 8%. HPMC is a gelling agent that can affect the antioxidant value contained in topical preparations. The method in making face serum preparations of pegagan (Centella asiatica L.) extract utilizing the combination of HPMC with chitosan which both have the property of influencing the antioxidant properties of serum preparations made and measurement of antioxidant activity using the DPPH attenuation method as measure by UV-Vis spectrophotometry. The serum of pegagan (Centella asiatica L.) extract which has the best antioxidant activity is Formula 1 (F1) with an IC50 value of 110 μg/mL. F1, F2, and F3 are categories of IC50 values ​​which are included in the category of having moderate levels of antioxidant activity.

PENINGKATAN DISOLUSI CELECOXIB MELALUI PEMBENTUKAN DISPERSI PADAT DENGAN HPMC-PEG 6000

ABSTRACTCelecoxib (CLX) is a drug that has low solubility and high permeability and belongs to BCS class II. The low solubility of CLX results in the bioavailability of CLX being only 40%, so it is necessary to increase the dissolution using a solid dispersion (DP) technique. This study aims to determine the dissolution profile of CLX in DP with a carrier combination of HPMC and PEG 6000. DP CLX were prepared by solvent evaporation method using drug-HPMC-PEG 6000 ratios were (1:1:1), (1:1:2) and (1:2:1). Pure CLX, physical mixture (CF) at the same ratio and DP were tested for dissolution in tribasic sodium phosphate 0.04 M (pH 12) and 1% sodium lauryl sulfate (SLS). The data from the dissolution test in the form of Q45 and DE60 values were analyzed statistically using non-parametric test. Overall Q45 DP CLX value > 75% and significantly different from pure CLX and CF. DE60 CLX value in DP ratio (1:1:1) 59.13±0.44%; ratio (1:1:2) 60.77±0.09%; ratio (1:2:1) 60.47±0.42%. Solid dispersion with a combination of HPMC polymer and PEG 6000 was able to increase the dissolution of celecoxib compared to the physical mixture and pure celecoxib.Keywords: celecoxib, dissolution, HPMC, PEG 6000, solid dispersion

Optimization of cardamom fruit ethanol extract gel with combination of HPMC and Sodium Alginate as the gelling agent using Simplex Lattice Design

Abstract Background: Cardamom has been studied and proven to be effective as an antibacterial. Gel preparations are preferred because they have advantages such as being easy to apply, providing a cooling effect, and being able to deliver drugs well. Objective: The purpose of this study was to make a gel formulation of ethanolic cardamom fruit extract by optimizing the combination of the gelling agent of HPMC and sodium alginate using the simplex lattice design (SLD). Methods: Cardamom fruit extract was obtained by extracting cardamom fruit simplicia using 70% ethanol. The formulation of the gel preparation from cardamom fruit extract was optimized using the SLD method on Design Expert. There were 5 gel formulas made and evaluated including organoleptic, pH, viscosity, spreadability, and adhesion. The independent variables in SLD were the amount of HMC and sodium alginate, while the responses included viscosity, spreadability, and adhesion. Optimal formula selection is done by using a numerical approach. Results: FI (HPMC 3.75% and sodium alginate 2.75%) and FII (HPMC 3.50% and sodium alginate 3.00%) met the test criteria for all the tests performed. The optimal formula suggested by SLD is a combination of 3.53% HPMC and 2.98% sodium alginate with a desirability value of 1.00. The predicted value for each response was the viscosity of 214.83 dPa.s, dispersion of 5.38 cm, and adhesion of 50.08 seconds. The optimal formula showed a dispersion value of 5.37cm. The results of the t-test indicated that the dispersion value of the observed results is not significantly different from the prediction software. Conclusion: Based on this research, it can be concluded that the use of a combination of HPMC and sodium alginate as a gelling agent can be optimized by using a simplex lattice design to obtain the optimum formula for cardamom fruit extract gel. Keywords: gel, hpmc, sodium alginate, SLD, kapulaga

OPTIMASI FORMULA PATCH KOSMETIK EKSTRAK METANOL DAUN PACAR AIR (Impatiens balsamina L.) DENGAN KOMBINASI MATRIKS HPMC DAN POLIETILEN GLIKOL 400 SECARA SIMPLEX LATTICE DESIGN

Pacar air leaves contain coumarin compounds, flavonoids, quinones, and saponins which are known to have antibacterial activity. The purpose of this study was to determine the optimum proportion of the combination of HPMC and Propylene Glycol 400 and to determine the antibacterial activity of the methanol extract patch of pacar air leaves. Extraction using the maceration method with methanol. Optimization is done using the simplex lattice design, tested for physical quality. The optimum formula is then verified using the T-test. Antibacterial activity test of patch preparations was carried out by looking at the size of the inhibition zone, the inhibition diameter data obtained were processed with ANOVA statistics. The results of this research were the patch formula with a combination of HPMC (11.25 grams) and PEG 400 (3.75 grams). PEG 400 cannot be used singly because it cannot be solid. The results of the activity test of the methanol extract of the leaves of water henna against the Staphylococcus epidermidis bacteria showed that the average diameter of the inhibition zone was 15.16 ± 0.75mm. The results of one way ANOVA test obtained data of 0.096> 0.05, indicating that the positive control with the sample was not significantly different.

OPTIMASI KOMBINASI HPMC DAN CARBOPOL DALAM FORMULA SEDIAAN GEL HAND SANITIZER EKSTRAK ETANOL BIJI PEPAYA (Carica papaya L.) SERTA UJI AKTIVITAS ANTIBAKTERI TERHADAP Escherichia coli

Papaya seeds (Carica papaya L.) have antibacterial activity because they contain terpenoid, karpain and flavonoid compounds. Flavonoids have OH groups that can damage bacterial cell walls. The dry powder of papaya seeds was extracted by maceration method using 80% ethanol. The purpose of this study was to determine the optimal combination of HPMC and carbopol concentrations in the hand sanitizer gel of papaya seed ethanol extract which can influence the in vitro inhibition of Escherichia coli bacteria. The data analysis used in this study was one way ANOVA and then continued with the Post Hoc Tests. The results of the study obtained a yield of 6.933%. The optimum formula obtained is RUN 8 with a concentration of HPMC: Carbopol (0.25gram: 0.75gram). The results of antibacterial activity against Escherichia coli bacteria obtained an average of 44.25 mm from the two samples. The statistical results obtained stated that there was no significant difference between the concentration of A and ciprofloxacin as a positive control.

Supersaturated LFCS type III self-emulsifying delivery systems of sorafenib tosylate with improved biopharmaceutical performance: QbD-enabled development and evaluation.

The current studies investigate the application of quality by design-enabled type III self-emulsifying delivery system (Type III-SEDDS) of sorafenib tosylate (SFN) in improving its biopharmaceutical attributes. Initially, lipidic and emulsifying excipients were selected by carrying out solubility and phase titration experiments. After screening studies using Taguchi OA design, Type III-SEDDS were further optimised using D-optimal mixture design. The prepared formulations were assessed for globule size, zeta potential and percent of drug release. Following graphical optimisation, the optimum formulation was earmarked and further supersaturated to form saturated Type III-SEDDS (Sat-Type III-SEDDS) using a combination of HPMC and PVP to improve the stability of the formulation for a prolonged period. In vitro drug release of Type III-SEDDS study indicated approximately 8-fold improvement in dissolution rate over the pure powder drug. Cell uptake studies demonstrated higher uptake of dye-loaded Type III-SEDDS formulations in Caco-2 cells vis-à-vis plain dye. Cytotoxicity assay on Hep G2 cells revealed significant reduction in cell growth with Type III- and Sat-Type III-SEDDS vis-à-vis the pure drug. Furthermore, in situ permeation studies carried out using Wistar rats exhibited nearly 8.3- to 10.2-fold augmentation in permeation and absorption parameters of the drug from the Type III- and Sat-Type III-SEDDS, respectively, vis-à-vis the pure drug. Pharmacokinetic studies indicated nearly 3.98- and 3.62-fold improvement in AUC0-72, and 8.01- and 5.42-fold in Cmax, along with 0.25-fold decrease in Tmax of the drug from Type III- and Sat-Type III-SEDDS, respectively, in comparison with the SFN suspension. Furthermore, high degree of level A linear correlation was established between fractions of drug dissolved (in vitro) and of drug absorbed (in vivo) at the corresponding time points for Sat-Type III-SEDDS and pure drug, whereas the Type III-SEDDS exhibited a nonlinear relationship. Stability studies indicated the robustness of Sat-Type III-SEDDS, when stored at 25°C for 3months. Overall, the manuscript documents the successful systematic development of SFN-loaded Sat-Type III-SEDDS with distinctly improved biopharmaceutical performance. Graphical abstract.

FORMULATION AND EVALUATION OF LYCOPENE LOADED COLLOIDAL MICROPARTICLES GEL

Objective: The objective of the present investigation was to design and evaluate a gel containing lycopene loaded colloidal microparticles.
 Methods: The lycopene loaded colloidal microparticles were successfully prepared by Cloud point technique to form colloids using Tween 40 and Tween 60 surfactant solution and then incorporated into microparticles by solvent evaporation method using polymer like HPMC and ethyl cellulose. These colloidal microparticles were evaluated for particle size (PS), drug loading (DL), entrapment efficiency (EE), Scanning Electron Microscopy (SEM). Further, these colloidal microparticles were incorporated into a topical formulation i.e., gel. This topical formulation was then evaluated for macroscopic examination, viscosity, drug content, spreadability, antioxidant activity, in vitro permeation and release kinetics.
 Results: Colloidal microparticles were successfully prepared and the particle size, drug loading and entrapment efficiency were found to be 249.45±14.2 μm, 49.8±0.96 % and 93.4±0.26 % respectively. FTIR study depicted no chemical interaction between pure drug lycopene and other excipients. The topical formulation showed sustained release and followed Korsmeyer-Peppas release kinetics model.
 Conclusion: The sustained release topical formulation of lycopene was successfully prepared using Tween 40 and Tween 60 surfactant solution and combination of HPMC and ethyl cellulose and evaluated for several parameters.

Design and Evaluation of Transdermal Patches of Labetalol Hydrochloride

Introduction: β-blockers like labetalol hydrochloride (LHCl) are potent and highly effective antihypertensive agents. The main drawback associated with β-blockers is extensive first-pass metabolism, variable bioavailability requiring frequent dose administration. This makes them an ideal candidate for transdermal therapeutic systems. β-blockers formulated as transdermal therapeutic system should enhance the bioavailability as well as improve patient compliance. Constant innovations and improvement in this field have potential that large‐scale commercialization of transdermal dosage forms can be done. Aim: The aim of the present work was to develop and evaluate matrix type transdermal patches containing new polymeric combination to enhance the bioavailability as well as improve patient compliance. Materials and Methods: In present work development and evaluation of matrix-type transdermal patches containing a new polymeric combination of HPMC, carbopol934, ethyl cellulose, propylene glycol, polyethylene glycol, and isopropyl myristate for labetalol (LHCl) HCl (LBHCl). Film casting technique has been used in preparing patches. The patches were characterized for physical, in vitro release studies and ex vivo permeation studies using human cadaver skin. Result: F6 was found to be better than the other formulations and hence selected as the optimized formulation on the basis of results of evaluating parameters such as thickness, flatness, folding endurance, tensile strength, moisture content, moisture uptake, and drug content, formulation. The optimized patch was assessed for its pharmacokinetic, pharmacodynamic, skin irritation test and stability studies. Conclusion: Successful development of sustained release matrix type of transdermal patches which can show greater patient compliance in treating hypertension has been done.

PREPARATION, EVALUATION AND OPTIMIZATION OF MUCOADHESIVE MINI TABLETS OF TELMISARTAN BY USING SINGLE UNIT ENCAPSULATION SYSTEM

The objective of the present study was to develop and optimize capsule filled oral mucoadhesive minitablets of telmisartan. Wet granulation method was employed for the development of minitablets. All the formulations (F1- F13) exhibited more than 21% drug release at 4h and at the end of 12h it showed drug release more than 90%. During the dissolution study it was observed that the capsule shell in which the minitablets were filled got completely dissolved in the first 5 min. FTIR and UV study showed absence of any significant physical and chemical interaction between drug and polymers. Formulation F 10 was found to possess higher drug release at 4h and 12 h. Combination of HPMC and Carbopol was found to be suitable for formulation of mucoadhesive minitablets, showed promising mucoadhesive strength and exhibited controlled drug release over an extended period of time.