HPMC E5 Research Articles

Rosuvastatin, Perindopril and Ezetimibe loaded instant release buccal films: Development and in vitro characterization.

Rosuvastatin Calcium and Ezetimibe are used to control cholesterol level while Perindopril Erbumine is used to treat hypertension. Hepatic metabolism reduces the therapeutic effect of these drugs. Instant release buccal films (IRBFs) could possibly be a solution to this issue. The objective of the study was to formulate IRBFs of Rosuvastatin Calcium, Perindopril Erbumine and Ezetimibe using solvent casting technique. Polymers used to prepare IRBFs included hydroxypropyl methylcellulose (HPMC E5), PEG 400 (as plasticizer) and Tween 80 (as surfactant). Solvent casting technique was used to fabricate the films, followed by their in-vitro analysis including high performance liquid chromatography (HPLC), X-ray diffraction (XRD), fourier transform infrared evaluation (FTIR), In-vitro dissolution, In-vitro disintegration, stability tests, scanning electron microscopy (SEM), folding fortitude, thickness evaluation, surface pH, tensile strength, weight variation and percentage moisture content. Optical microscopy as well as SEM analysis displayed that the surfaces of IRBFs were smooth with uniform mixing of ingredients. IRBFs disintegrated within 15 seconds while on dissolution they exhibited instant drug release i.e. 100% release in 2 minutes. The results show promising potential of IRBFs in drug delivery.

Bioavailability Improvement of Carbamazepine via Oral Administration of Modified-Release Amorphous Solid Dispersions in Rats.

The purpose of this study was to improve the bioavailability of carbamazepine (CBZ), a poorly water-soluble antiepileptic drug, via modified-release amorphous solid dispersions (mr-ASD) by a thin film freezing (TFF) process. Three types of CBZ-mr-ASD with immediate-, delayed-, and controlled-release properties were successfully prepared with HPMC E3 (hydrophilic), L100-55 (enteric), and cellulose acetate (CA, lipophilic), defined as CBZ-ir-ASD, CBZ-dr-ASD, and CBZ-cr-ASD, respectively. A dry granulation method was used to prepare CBZ-mr-ASD capsule formulations. Various characterization techniques were applied to evaluate the physicochemical properties of CBZ-mr-ASD and the related capsules. The drug remained in an amorphous state when encapsulated within CBZ-mr-ASD, and the capsule formulation progress did not affect the performance of the dispersions. In dissolution tests, the preparations and the corresponding dosage forms similarly showed typical immediate-, delayed-, and controlled-release properties depending on the solubility of the polymers. Moreover, single-dose 24 h pharmacokinetic studies in rats indicated that CBZ-mr-ASD significantly enhanced the oral absorption of CBZ compared to that of crude CBZ. Increased oral absorption of CBZ was observed, especially in the CBZ-dr-ASD formulation, which showed a better pharmacokinetic profile than that of crude CBZ with 2.63- and 3.17-fold improved bioavailability of the drug and its main active metabolite carbamazepine 10,11-epoxide (CBZ-E).

Design and Development of Propranolol Hydrochloride Transdermal Patches: In Vitro and Ex Vivo Characterization

The main aim of this investigation is to design and develop matrix type transdermal patches of Propranolol Hydrochloride which is an anti-hypertensive drug. These matrix type transdermal patches were prepared by “Solvent Casting Technique” using drug, HPMC E15 and Eudragit L 100 in the ratio of 1:6, 1:6.5, 1:7, 1:7.5, 1:8, 1:8.5, 1:9, 1:9.5. All formulations carried 20%v/w of PEG-600 as plasticizer. The prepared patches were characterized for various physicochemical parameters like weight, thickness, folding endurance, drug content, percent moisture content, percent moisture absorption, in vitro drug release and ex vivo permeation. Among this 1:9 ratio was found to be an Optimized formulation and patches were prepared by using permeation enhancers (lemon grass oil, Eucalyptus oil, and clove oil). The cumulative amount of drug release in 12hrs for F7 formulation showed maximum and used for that formulation skin permeation on Goat abdominal skin. FTIR studies show no interaction between drug, polymer and other excipients. The drug permeation kinetics followed “First order” and “zero order” profile with diffusion mechanism.

Formulation and Evaluation of Film Forming Gel of Mometasone Furoate

The present investigation was aimed to formulate and evaluate film forming gel of Mometasone furoate by dispersion method with HPMC E15, Carbomer 934 and propylene glycol to increase the drug penetration through the skin. The gelling agent was dispersed in solvent with stirring at 1200 RPM for 30mins. Drug was dissolved in non aqueous solvent followed by addition of preservative and flavouring agent. The prepared formulation was evaluated for invitro diffusion study release, spreadability etc. All formulation showed drug release from 51.79% to 97.89%, good homogeneity and gel was easily spreadable. Optimized formulation showed enhanced rate of diffusion, drug release and was found suitable for sustained release with good stability.

Biomimetic micellar mesoporous silica xerogel performs superior nitrendipine dissolution, systemic stability and cellular transmembrane transport.

To combine the advantages of micelles and biomimetic silica materials, biomimetic micellar mesoporous silica xerogel (BM-SX) was initially established, biomimetic silica xerogel (B-SX) was also studied as control and nitrendipine (NDP) was taken as model drug. The content mainly focused on drug dissolution, systemic stability and cellular transmembrane transport of NDP loaded B-SX and NDP loaded BM-SX. With extra mesopores formed due to HPMC E50 micelles, the mean pore diameter, surface area and pore volume of BM-SX were all larger than B-SX. After loading NDP into the two carriers, crystal NDP changed to amorphous phase, leading to enhanced NDP dissolution. BM-SX presented superior abilities not only for its higher drug dissolution compared to B-SX but also for its capacity in remaining high amorphous drug phase and therefore no drug dissolution reduction can be observed. The dynamic contact angle result confirmed the strong power of HPMC E50 micelles in maintaining amorphous NDP in the carrier to improve high systemic stability. Both B-SX and BM-SX could increase drug absorption permeability and exert function as drug efflux inhibitor to inhibit the efflux effect of p-gp drug pump and promote NDP absorption and transport, and BM-SX was superior owing to micelles in the system.

Application of Central Composite Design for Citalopram Hydrogen bromide Mouth Dissolving Films

Citalopram is an antidepressant used for treating major depressive disorder. In the current work Citalopram HBr is formulated as mouth dissolving film with enhanced drug dissolution. The Central Composite Design (CCD), employed to examine the effects of amount of HPMC E50 (A), amount of maltodextrin (B) and amount of glycerol (C) on response variables tensile strength, disintegration time and cumulative % drug release. 27 formulations prepared according to CCD and evaluated for physicochemical parameters and in vitro dissolution studies. Citalopram HBr mouth dissolving films formulated by employing solvent-casting method using HPMC E50, maltodextrin and glycerol, optimized for the effective dosage of superdisintegrants. The formulation CF21 with maximum tensile strength of 67.21±1.31 gm, least disintegration time of 9±1.60 sec and highest drug release of 98.41±1.81% is chosen optimal formulation with maximum content uniformity and folding endurance. It is evident from the above results that the developed formulation can be an innovative dosage form to improve the drug delivery, quick onset of action as well as improve patient compliance in the effective management of depression.

The effect of particle size on dissolution rate of fast dissolving oral film containing diclofenac sodium

Diclofenac sodium is a Non-Steroidal Anti Inflammatory Drugs that if being taken orally have the side effects of peptic ulcers and undergone the first pass metabolism, and also included in the Biopharmaceutics Classification System class 2 which resulted in the low rate of dissolution. This study aims to determine the influence of particle size reduction on the dissolution rate of diclofenac sodium in the form of an FDOF dosage. The formation of diclofenac sodium nanoparticles is carried out by ionic gelation method using chitosan and sodium tripolyphosphate as a crosslinker in various ratios characterized by Particle Size Analyzer and Scanning Electron Microscopy, then it is incorporated into the form of an FDOF that were prepared by solvent casting method at a dose of 12.5 mg using variations concentration of SSG as superdisintegrant and PEG 400 as plasticizer. From the research results, diclofenac sodium nanoparticles are formed in the ratio of chitosan-sodium tripolyphosphate 6:1, have a size of 804 nm and spherical-shaped. The best FDOF dosage formula is F8 containing HPMC E5 LV 35% as the film forming agent, SSG 8% as superdisintegrant and PEG 400 10% as plasticizer. FDOF formula containing diclofenac sodium nanoparticles has a slightly bitter taste, disintegration time less than one minute, surface pH around 7 (neutral), drug content that meets the requirements of the range of determination which is 93.24 ± 0.96, the cumulative amount of drug dissolved in the 28th minute is higher by 88.45% compared to FDOF containing diclofenac sodium raw material, which is only 70.0%.

DESIGN AND DEVELOPMENT OF FLOATING PULSATILE DRUG DELIVERY OF LOSARTAN POTASSIUM

Objective: The objective of the present investigation was to the development of floating pulsatile drug delivery system of Losartan potassium (LP) tablets for obtaining no drug release during floating followed by pulsed, rapid drug release to achieve chronotherapeutic release. In hypertension, the risk of getting heart attacks early in the morning is high and therefore, there was need to develop drug delivery, which will release drugs at morning hours and provide efficacious therapy. LP is a short biological half-life (1.5-2.5h) and readily absorbed from the stomach and upper gastrointestinal tract.
 Methods: Tablet formulation was prepared by press coating of rapid release core tablets and core tablets were further top coated with a buoyant layer of HPMC K4M and sodium bicarbonate. Various grades of HPMC polymer (E5/E15/E50) were used for the pulsatile coating layer. The developed formulations were characterized for physical characteristics, floating lag time, floating time, release lag time, drug content, swelling index, in vitro dissolution studies, DSC and XRD.
 Results: The FTIR and DSC studies predicted that there was no chemical interaction between drug and excipients. The core tablet coated with HPMC E50 showed a high swelling index and release the drug 97.60±1.2% at 6h. Buoyant layer with 80 mg HPMC K4M and 25 mg sodium bicarbonate gave satisfactory floating lag time.
 Conclusion: The system showed an excellent lag phase followed by burst release in the distal small intestine, which gives site and time-specific delivery of LP acting as per chronotherapy for treatment of hypertension.

Comparison Between the Pharmacokinetics Data of Ketorolac Tromethamine Wafer a Novel Drug Delivery System and Conventional Ketorolac Tromethamine Tablets to Enhance Patient Compliance Using a New LC-MS/MS Method

Ketorolac tromethamine (KTM) is a potent and widely used non-steroidal anti-inflammatory drug. Despite its efficacy, it causes gastric irritation and increases the risk of gastrointestinal injuries. This study aimed to formulate KTM wafer to overcome its harmful gastrointestinal side effects. By solvent evaporation method six formulae prepared with different concentrations of polymers of sodium carboxymethyl cellulose, sodium alginate, and hydroxypropyl methylcellulose (HPMC E15). The formula F2 with high concentration of sodium alginate wafer, shows disintegration time in 85 s, with pH 6.6,% drug loaded with 102% and high dissolution release rate in 20 min. Drug release pattern appears to be second order. The mean Cpmax values of F2 wafer and the marketed product were 2135.47 ± 13.83 ng/mL and 1073 ± 23.5, respectively. The median values of Tmax were 1 and 3 h, respectively. The calculated AUC0 − ∞values were 2087 ± 71.58 and 3981 ± 62.34 ng h/mL for F2 and marketed product, correspondingly. The relative bioavailability was found to be 0.52. A new rapid, sensitive, and specific LC-MS/MS fully validated method was developed for the determination and quantification of KTM, using torsemide as internal standard, in biological sample. It was successfully applied to perform the pharmacokinetic and the bioavailability study.

A Design of Experiment (DoE) based approach for development and optimization of nanosuspensions of telmisartan, a BCS class II antihypertensive drug

BackgroundThe present study was aimed to enhance the solubility and dissolution of BCS class II drug, telmisartan (TEM), by nanoformulation approach. Several attempts were made to develop a nanosuspension by bottom-up and top-down techniques. In our study, we found in situ nanoamorphization technique to be incompatible and hence was not selected for further development of nanoformulation. Bottom-up techniques such as anti-solvent precipitation and emulsification solvent evaporation methods failed to reduce the size of the drug to nanoform by HPMC E15 and PVP K-25 at 1500–2000 rpm but resulted in micron-sized particles.ResultsHowever, the acid-base neutralization method has produced nanosuspension with a particle size of 243.9 nm and 0.119 PDI. Formulation and analytical development were carried out by statistical factorial design using the Design-Expert software (version 11.0). The nanosuspensions remained stable even after 90 days without any aggregations with particle size 338.1 nm and PDI 0.146. Zeta potential of optimized formulation was found to be − 16.2 mV. Drug content and its release were estimated by the developed and validated in-house HPLC method. In vitro drug diffusion studies on the optimized formulation have shown a drug release of 82.6% by the end of 3 h, whereas plain drug suspension has shown only 42.8% release, indicating a 2-fold increase of drug diffusion with nanosuspension. Ex vivo drug permeation studies performed using excised goat gastric mucosa revealed much faster permeation of TEM from nanosuspension than the plain drug suspension.ConclusionsHence, from the results, it can be concluded that TEM, when formulated by acid-base neutralization method as a nanosuspension, leads to enhanced solubility, dissolution, and stability.

A Review on Precipitation inhibitors in supersaturable self emulsifying drug delivery system

The super saturable formulation has been widely used as an effective method to improve solubility and oral absorption of poorly aqueous-soluble drugs. When the super saturable formulation comes in contact with gastrointestinal fluids, its drug concentration goes over the equilibrium solubility, but this state does not exist for too long, the drug may precipitate before being absorbed, which minimizes the efficacy and bioavailability of the drug. Therefore, it is necessary to inhibit or retard the precipitation of drugs to achieve the maximum benefits of the super saturable formulation. Polymers (watersoluble and insoluble) are the commonly used excipients to inhibit precipitation. Cyclodextrins and surfactants are the other two excipients used as precipitation inhibitors. In some of the cases, even solid carriers can effectively retard precipitation. The precipitation inhibitors (PI) have the capacity to maintain a super saturable state of the formulation in GI for a particular time period. Therefore, it is important to properly select the precipitation inhibitor; too frequently used methods to select precipitation inhibitor are casting film method and solvent-shift method. Such selected and successfully used precipitation inhibitors are HPMC E5LV, PVP K17, HPMC E5, soluplus, poloxamer 407, HPMCAS, maltodextrin (mal) and microcrystalline cellulose (mcc). Since the super saturable technique has been widely used for delivering poorly water-soluble drugs like ezetimibe, indirubin, feno fibrate, butyl paraben and rosu vastatin calcium. There is a necessity for bio relevant evaluation of supersaturation/precipitation because simple methods like dissolution tests cannot be bio relevant in a supersaturation/precipitation context. Some of the important factors like sink versus non-sink conditions, hydrodynamic, medium selection and temperature play a vital role in the evaluation of in-vitro supersaturation

FORMULATION OPTIMIZATION AND EVALUATION OF MOUTH DISSOLVING FILM OF RAMOSETRON HYDROCHLORIDE

Objective: Ramosetron Hydrochloride is found to be more potent and having a longer duration of action with the least side effects, but the major drawback is it undergoes hepatic first-pass metabolism so our aim is to prepare mouth dissolving film (MDF) of Ramosetron hydrochloride for rapid relief in emesis.
 Methods: The mouth dissolving films of Ramosetron Hydrochloride were prepared by using the solvent casting method. Films were formulated using HPMC E5 (Hydroxy Propyl Methyl Cellulose) as a film-forming agent, PEG400 (Polyethylene glycol) as a plasticizer and Aspartame as the sweetening agent. A 32 full factorial design was applied considering the concentration of HPMC E5 (X1) and concentration of PEG400 (X2) as independent variables and % cumulative drug release (Y1) (CDR), disintegration time (Y2) (DT) and tensile strength (Y3) (TS) as dependent variables. The prepared films were evaluated for thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and taste masking by E-tongue. The results indicated that factors X1 and X2 were found to be having a positive effect on DT and TS and negative effects on CDR.
 Results: The optimized formulation was found to be the best with 94.00±0.85% in vitro drug release, 33.22±0.75 sec DT and 1.359±0.005 g/mm2 tensile strength. Concentration of aspartame was optimized with E-tongue taking into consideration increased electric potential with decreasing bitterness.
 Conclusion: Thus, a rapidly dissolving oral film of Ramosetron Hydrochloride with successful taste masking and immediate in vitro drug release was prepared using a solvent casting technique.

Enhanced pharmacokinetic performance of dapoxetine hydrochloride via the formulation of instantly-dissolving buccal films with acidic pH modifier and hydrophilic cyclodextrin: Factorial analysis, in vitro and in vivo assessment

Instantly dissolving buccal films have gained attention owing to their easy administration and capability to surmount the hepatic first pass effect of drugs. Dapoxetine hydrochloride (DPX) has a low oral bioavailability due to significant hepatic first pass metabolism. In addition, DPX is a weakly basic drug with a pH dependent solubility that could limit its dissolution in the body neutral fluids. In order to surpass these challenges, this work aimed at enhancing DPX bioavailability via the formulation of instantly dissolving buccal films comprising a pH modifier and a hydrophilic cyclodextrin. Tartaric acid and hydroxypropyl beta-cyclodextrin were selected as dual solubilizing agents based on the screening study. 32 factorial design was employed for the formulation and optimization of DPX films. Statistical analysis revealed that hydroxypropyl methyl cellulose E5: maltodextrin ratio and propylene glycol concentrations have significant effects on mechanical properties, percent DPX dissolved after 5 min, and in vivo mouth dissolving time at P < 0.05. The optimized film [HPMC E5: MDX, 1:1 and 1% PG] showed no significant change of properties or drug dissolution upon storage at 40 °C/75% RH for a period of 3 months. In addition, the optimized film showed significantly enhanced absorption relative to the oral reference tablet. Therefore, the optimized film could be considered a promising delivery system for DPX with expected improved patient compliance and enhanced pharmacokinetic performance.

Development and optimization of osmotically controlled drug delivery system for poorly aqueous soluble diacerein to improve its bioavailability

In an attempt to improve the low oral bioavailability of Diacerein (DCN), the combination of a ternary solid dispersion and an asymmetric osmotic pump system had been designed to enhance solubility and to control DCN delivery. Ternary DCN solid dispersion was prepared by melting fusion method using surfactant polymers, and carrier (Pluronic® PF127, Solutol® HS15, and PEG 35 K) and this DCN solid dispersion powder with the proper amount of excipients were compressed and coated with Opadry®CA to develop a Semi-Permeable and Asymmetric Osmotic Pump tablets. The ternary DCN solid dispersion by using surfactant polymers (Pluronic® F127 and Solutol® HS 15) with a ratio of 1:1 was displayed market significant improvement in saturated solubility (70.2 ± 4.14 µg/ml) and fast dissolution rate (Q60min = 79.28 ± 3.1% and IDR5 min = 5.25 ± 0.19 ml/min) in comparison to pure DCN. Moreover, the optimized asymmetric osmotic pump tablet with following parameters; 3% w/v Opadry® CA coat concentration, 1% w/w HPMC E15 gelling polymer and 35.8%w/w NaCl Osmogen concentration, was displayed control release of DCN at zero-order kinetic (R2 = 0.977) for up to 24 h(s). The in-vivo study conducted on rabbits was revealed a significant enhancement in the bioavailability of the optimized osmotic pump (28.84 ± 3.32 ng.hr/ml) compared to DCN dispersion (10.39 ± 1.45 ng.hr/ml). In conclusion, the approach of enhancing solubility and wet-ability in accompany with optimized asymmetric osmotic pump system could serve as a promising delivery system and a way to improve the bioavailability of poorly aqueous soluble drugs.

Thin layer chromatographic compatibility study in preformulation of new transdermal therapeutic systems

Abstract Objective: The compatibility of four binary active substances combinations adapalene – levofloxacin (ADP-LFX), adapalene – miconazole nitrate (ADP-MCZ), levofloxacin – meloxicam (LFX-MLX) and levofloxacin – miconazole nitrate (LFX-MCZ) was analysed to be comprised in new transdermal therapeutic systems. Also, the compatibility of selected active substances and four polymeric excipients (hydroxypropyl methyl-cellulose - HPMC 15000, hydroxypropyl methylcellulose - HPMC E5, ethyl cellulose - EC 10, and hydroxyethyl cellulose – HEC) was studied. Methods: Thin layer chromatographic method (TLC) and four selected mobile phases were used. On the plate (in situ) were obtained the binary combinations (active substances and active substance-polymer). Results: A good compatibility of ADP-LFX was found using ammonia : methanol : acetonitrile : methylene chloride 2:4:1:4 mobile phase. Using chloroform : acetone : glacial acetic acid 34:4:3 on the chromatogram of ADP-MCZ, only ADP spots appeared but without changes in the shape of the spots and Rf values. Any modifications of LFX and MLX spots (from LFX-MLX mixture) had been observed using toluene : glacial acetic acid : methanol 11:1:0.5 mobile phase, although LFX spots have remained on the baseline. Only LFX spots were visible from LFX-MLX and LFX-MCZ mixtures (ammonia : methanol : acetonitrile : methylene chloride 2:4:1:4 mobile phase). Distinctive spots were observed for ADP, LFX and MLX with variable results from no chemical interactions to limited chemical interactions when the compatibility with polymers was verified. Conclusions: ADP-LFX and LFX-MLX mixtures were found to be compatible. ADP with HPMC polymers and LFX with HPMC E5 and HEC had presented excellent compatibility; for the other binary combinations, different analytical methods will be necessary.

A novel and innovative drug delivery system in fast dissolving oral film of glimepiride-betacyclodextrin inclusion complexes

Delivery system in fast dissolving oral film is the system in which drug can be released immediately without drinking water and can be dissolved in saliva, then absorbed into the body through the oral cavity. Glimepiride is classified in the Biopharmaceutics Classification System class II which has a low solubility in water. Formation of glimepiride inclusion complexes using betacyclodextrin is known to increase solubility while suppressing the bitter taste of glimepiride. The purpose of this study was to develop FDOF preparations containing glimepiridebetacyclodextrin (1:2) inclusion complexes made by co-grinding technique. The development of the FDOF formula begins with the orientation of the formula which varies the concentration of crospovidone as superdisintegrant and PEG 400 as plasticizer. The FDOF were made from two formulas, with one formula containing glimepiride-betacyclodextrin (1:2) inclusion complexes and the other formula containing pure glimepiride as the active ingredient, using the solvent casting method with HPMC E5 LV as the film forming agent. The final evaluations of FDOF include organoleptic, weight variation, film thickness, surface pH, disintegration time, drug content, dissolution rate, percent elongation, tensile strength and folding endurance tests. The best FDOF formula from optimization process contain HPMC E5 LV 35% as film forming agent, PEG 400 15% as plasticizer and 8% crospovidone as superdisintegrant. From the results of final preparation evaluation, FDOF containing glimepiride-betacyclodextrin (1:2) inclusion complexes proved to be better than FDOF containing pure glimepiride.

FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design.&#x0D; Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study.&#x0D; Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation.&#x0D; Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

Viscosity Effects of Hydrophilic Polymers on Transport of Collagen Hydrolysate Across Reconstructed Human Buccal Tissue

Herein we investigate the influence of hydrophilic polymers on the buccal permeability of collagen hydrolysate (CGH) by performing in vitro buccal permeation test and viscosity measurements. After we demonstrated that CGH (2000–3000 Da) could be delivered across the reconstructed human buccal tissue as evaluated by hydroxyproline assay, the effects of different hydrophilic polymers, varying amounts of CGH, and hydration methods were examined to elucidate the relationship with buccal permeation behavior of CGH. The percentage of CGH permeated was found to be highest in HPMC E5 solution and greater when the viscosity of test solutions was low. Using commercially obtained CGH‐loaded buccal films, the films under higher hydration condition exhibited greater CGH permeation. This study demonstrates that CGH can be delivered via the human buccal tissue and viscosity of the solution significantly affects the CGH permeation. These findings are valuable for designing hydrophilic polymer‐based buccal film formulations for peptides like CGH.

Formulation and evaluation of sitagliptin buccal patch

The aim of present work was to formulate and evaluate Sitagliptin buccal patch using solvent casting method. Buccal patch gained importance as it overcomes the limitations of current routes of administration, provides rapid onset of action by releasing drug directly to systemic circulation through oral mucosa by mucoadhesion. The formulated buccal patches were evaluated for various parameters like film thickness, surface pH, folding endurance, weight variation, % moisture loss, tensile strength, % elongation, drug content uniformity, and in vitro dissolution studies The optimized formulation (F4) containing HPMC E5 and Eudragit RL 100 polymer combination in 1:1 ratio showed highest in vitro dissolution (99.7 %) and satisfactory stability.

Development of scopolamine hydrobromide orodispersible films as an anti-sialagogue in dentistry: Optimization and in vitro evaluation

Scopolamine hydrobromide is the hydrobromide salt form of scopolamine and has anticholinergic, antiemetic and antivertigo properties. Its property of reducing the saliva secretion also reported. Orodispersible films are solid dosage forms, which disintegrate or dissolve within a minute when placed in the oral cavity. In order to overcome the drawback of the conventional scopolamine hydrobromide solution as antisialagogue we formulated the scopolamine hydrobromide orodispersible films by solvent casting method using pullulan and HPMC E15 polymer combination. The formulations were statistically optimized by full factorial design (32) using Design Expert® software. The optimized formulations were evaluated in vivo. The optimized formulations exhibited acceptable physical characteristics with good flexibility, folding endurance, tensile strength. As anticipated, the optimized scopolamine hydrobromide orodispersible films exhibited quick disintegration and drug release. From the in vitro disintegration and drug release study it was observed that the formulation F1 disintegrated in 9 ± 1 sec and ~98.37 drug was release at the end of 120 sec. Hence the scopolamine hydrobromide orodispersible films successfully tailored for the use in dentistry as an antisialagogue formulation.