Percentage Moisture Absorption Research Articles

Intravitreal Implantable Film Containing Ketorolac Tromethamine Microsponges – In Vitro/In Vivo Correlation

This research involved preparation, optimization, in vitro and in vivo evaluation of Ketorolac Tromethamine (KT) from the implantable film containing KT-microsponges to be inserted at the posterior part of the eye and may treat some complicated conditions such as cystoid macular edema (CME) and/or diabetic macular edema (DME). Specific amount of our previously prepared KT microsponges (equivalent to 6 mg KT) was added to a film base composed of poly vinyl alcohol (PVA) and glycerol to which 3 mg uncoated (pure) KT added then casting the combination to get film (0.6 cm × 0.3 cm). The prepared film was evaluated for weight uniformity, thickness, folding endurance, surface pH and the percentage of moisture absorption (PMA) and percentage moisture loss (PML) as well as in vitro release and in vivo tests. The obtained film showed average weight (8.87mg ± 0.2) with variation less than (5%), thickness (0.3 cm ± 0.04), surface pH ranged (7-7.3), folding endurance more than (300) times indicating excellent elasticity with good integrity through measuring percentage moisture absorption (PMA) and percentage moisture loss (PML). The in vitro release showed biphasic release where 40% of the drug was released within the first day (initial phase) followed by sustained release continued to give 90% of the drug within 3 months. The in vivo test showed that the implanted film in the vitreous chamber of the rabbit eye had good ant-inflammatory properties against acute and chronic inflammation as well as prevent recurrent inflammation. The work succeeded to prepare KT film containing microsponges to be implanted intravitreally at the posterior chamber of the eye and suggested to treat complicated condition including postoperative cystoid macular edema as well as diabetic macular edema as alternative to repeated intravitreal KT injections, so decreasing side effects with improved patient compliance.

Preparation and Evaluation of Sulfacetamide Sodium Ocusert for Controlled Drug Delivery

The intent of this research was to formulate and evaluate controlled release ocusert of sulfacetamide sodium for the treatment of bacterial conjunctivitis. Ocusert is a sterile preparation having drug as dispersion or as solution in the polymeric base. Prepared Ocuserts were formulated using hydroxyl propyl methyl cellulose K-15 and Ethyl cellulose as polymers at various concentrations and combinations. Polymeric Films were prepared by mercury casting method using different ratios of polymers. Selected physiochemical properties such as thickness, weight, percentage moisture absorption, and in-vitro release and sterility studies of sulfacetamide sodium ocusert were studied and reported that prepared ocusert resolved the problems of poor bioavailability, frequent dosing and wastage of active ingredient.
 Keywords: Hydroxypropyl methyl cellulose K-15, ocusert, sulfacetamide sodium

Preparation and Evaluation of Eudragit® L100 Nanoparticles Loaded Impregnated with KT Tromethamine Loaded PVA -HEC Insertions for Ophthalmic Drug Delivery.

Purpose: The purpose of the present study was to improve the ocular delivery for ketorolac tromethamine (KT) used to treat inflammation of the eye. Methods: Eudragit nanoparticles loaded with KT were prepared and incorporated in polyvinyl alcohol (PVA) and hydroxyethyl cellulose (HEC) films. Nanoparticles were characterized by Fourier transform-infrared (FT-IR), scanning electron microscopy (SEM). Physicochemical properties and encapsulation effciency were investigated for nanoparticles. Also, the inserts were evaluated for their physiochemical parameters like percentage moisture absorption, percentage moisture loss, thickness and folding endurance. Results: Mean particle size and zeta potential were in range of 153.8-217 nm and (-10.8) - (-40.7) mV, respectively. The results show that the use of a surfactant has not led to any major change on drug loading. The loading increases with the amount of polymer. The insert had a thickness varying from 0.072 ± 0.0098 to 0.0865 ± 0.0035 mm. The thicknesses of the inserts and the folding endurance increased with the total polymer concentration. The physicochemical properties showed that the Eudragit® L-100 nanoparticles loaded PVA-HEC films could be an effective carrier for KT. Conclusion: For the first time, inserts of Eudragit nanoparticles were successfully prepared for ophthalmic drug delivery system to prevent frequent drug administration and enhance patient compliance.

OPTIMIZATION AND PREPARATION OF SOLID LIPID NANOPARTICLE INCORPORATED TRANSDERMAL PATCH OF TIMOLOL MALEATE USING FACTORIAL DESIGN

Objective: Transdermal patch of timolol maleate was prepared in order to increase the permeability of the drug topically.
 Methods: The timolol maleate (TM) loaded solid lipid nanoparticles (SLN) were prepared by the solvent evaporation method. For the optimization process full factorial (three-factor and three-level), hydroxypropyl methylcellulose (HPMC) range from 100 to 300 mg, ethylcellulose 100 to 200 gm and almond oil 3 to 4 ml. The response noted in form of tensile strength and percent drug release. These transdermal patches were evaluated for physical characterization like weight variation, thickness, percentage moisture absorption, percentage moisture loss, water vapor transmission rate, folding endurance, tensile strength, and content uniformity.
 Results: Solid lipid nanoparticles of TM were optimized and prepared, the data presented that drug release percent ranged from 66.12 to 91.75. 2FI model was observed to fit for response % drug permeation with a p and F value of 0.0271 and 4.50. The tensile strength varies from 0.358 to 0.508. The linear model was observed to fit for the tensile strength response with a p-value and F-value of<0.0001 and 52.41.
 Conclusion: The controlled release formulation of Timolol Maleate was successfully optimized and prepared, a study conducted to investigate the effect of different polymers and type of permeation time profiles from Timolol Maleate patches.

FORMULATION OF MUCOADHESIVE BUCCAL FILMS USING PREGELATINIZED CASSAVA STARCH PHTHALATE AS A FILM-FORMING POLYMER

Objective: This study aimed to compare the characteristics of four buccal films formulated with phthalylated cassava starch and their drug deliverypotentials.Methods: An alternative to conventional (oral) drug administration is to administer drugs in a buccal film; however, the required dosage mustbe dissolved in a film-forming polymer with suitable mechanical and mucoadhesive characteristics. Previous studies have produced excipientsby physically and chemically modifying starch, such as by completely pregelatinization and phthalylation it in an aqueous medium under alkalineconditions (pH 8–10). This produced a pregelatinized cassava starch phthalate (PCSPh) powder with a high degree of substitution (0.0541±0.0019),thus giving it different physical, chemical, and functional characteristics than unphthalated PCS.Results: PCSPh in 4.5% and 6% (w/w) concentrations was used as excipients for producing four formulations of buccal film. One film had themost suitable characteristics, with an ex vivo mucoadhesion time of 57.1±20.3 min, tensile strength of 0.84±0.02 N/mm2, and a more rapid drugrelease profile than two of the other film types produced. Our tests also revealed that the best film tended to not change physically when moistened(percentage moisture absorption was 139% and moisture loss was 65%).Conclusion: Thus, we predict that PCSPh could be adequately formulated to provide mucoadhesive buccal films with an appropriate drug release profile.

EVALUATION OF OCULAR FILMS OF OFLOXACIN FOR ANTIBACTERIAL ACTIVITY

Objective: The current study emphasizes on the treatment of ocular infection with objectives of reducing the frequency of administration, obtaining controlled release and greater therapeutic efficacy of the drug (ofloxacin) using ocular films.Methods: Ocular films were designed by solvent evaporation method containing a different combination of polymers. The folding endurance (mechanical strength) was determined by the number of folds at a specific single place required to break the film into two parts. Thickness was measured using screw gauze. The surface pH was done by pH paper. The percentage moisture absorption was carried out by placing the ocular films in a desiccator containing ammonium chloride. Percentage moisture loss was carried out by placing the ocular films in the desiccator containing anhydrous calcium chloride. in vitro drug release study were carried by using a modified version of franz diffusion cell. Stability study were carried using stability chambers as per ICH guidelines. The antibacterial activity was performed by using male albino rabbits.Results: The thickness and folding endurance of the films were in the range of 44±1.1 to 92±1.8 and 4.5±0.6 to 6.8±0.3, respectively for different formulations. Surface pH was evaluated in the range of 6.6 to 7.2. Percentage moisture absorption and percentage moisture loss were evaluated in the range of 1.17±1.1 to 6.72±1.5 and 0.58±0.9 to 1.23±0.9 respectively. Microbial growth was not observed in any formulation during sterility testing. The drug release for different batch codes PAH, PBE, PCP, PDC, PEEH, and PFEC was found to be 96.2, 56.9, 93.4, 94.5, 98.4 and 95.9 % respectively up to 12 h. Ocular films of batch code PEEH was optimized for maximum drug release (98.4%). The antibacterial effect was noted periodically (01 to 05 d) after administration of sterile formulation in the treated eyes vs. control eyes of each rabbit. The optimized batch PEEH of ocular films reduced the infection and redness completely within 3 d in a single dose.Conclusion: The optimized formulation would be able to offer benefits such as increased residence time, prolonged drug release, reduced frequency of administration and improved patient compliance with complete removal of inflammation and redness from the cul-de-sac.

Barrier property enhancement of starch citrate bioplastic film by an ammonium-thiourea complex modification

Although citric acid modification of starch biopolymers gives a more thermodynamically stable starch citrate, the barrier properties of the product is relatively poor. This paper reports a novel modification process which significantly improved the barrier properties of starch citrate by treating it with a complex formed from ammonium acetate and thiourea in the presence of a polysorbate catalyst. The barrier characteristics which were investigated include percentage moisture absorption, percentage reflectance, and water vapour release study. FTIR, SEM and TGA were employed to characterize the starch citrate biofilms before and after ammonium-thiourea complex modifications.

FORMULATION AND CHARACTERIZATION OF PERIODONTAL FILMS CONTAINING AZITHROMYCIN AND SERRATIOPEPTIDASE

Objective: The objective of the present work was to formulate and evaluate periodontal film, which could be capable of delivering therapeutic concentration of azithromycin and serratiopeptidase for a prolonged period of time and could be easily placed into the periodontal pocket. Methods: The films were prepared by solvent casting method using combinations of ethyl cellulose, hydroxypropyl methylcellulose K4M, hydroxypropyl methylcellulose 50 cps, eudragit L-100, and Chitosan in different ratios using dibutyl phthalate as plasticizer. The periodontal films were evaluated for weight variation, thickness, percentage moisture absorption, percentage moisture loss, folding endurance, percentage swelling index, percentage elongation, and in vitro percentage cumulative drug-enzyme release profile. Results: Formulation F12 was found to be a good periodontal film. Hence, it was considered as an optimized formulation. In vitro drug-enzyme release rate studies using keshary-chien diffusion cell showed maximum drug release in F12 formulation (95.92% for azithromycin and 94.20% for serratiopeptidase at the end of 24 h) compared to other formulations. Conclusion: The optimized formulation F12 showed the best drug-enzyme release profile among the others for the preparation of periodontal film. There is a scope for the further study and development of the azithromycin and serratiopeptidase periodontal films.

Solid Dispersion Incorporated Fast Dissolving Oral Wafers of Cinnarizine: Development and Evaluation

Cinnarizine is a piperazine derivative, antiallergic with antihistamine, sedative, and calcium-channel blocking activity. It is used for the symptomatic treatment of nausea and vertigo caused by Meniere’s disease and other vestibular disorders and for the prevention and treatment of motion sickness. The present study is focused on making fast dissolving wafers of solid dispersion incorporated Cinnarizine to enhance the bioavailability, dissolution of the drug and increasing the patient compliance. Fast dissolving films of Cinnarizine can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action is desirable along with the convenience of administration. Seven formulations of fast releasing wafers of solid dispersion incorporated Cinnarizine, dispersed in two different polymers; HPMC and PVA by solvent casting method were prepared. Solid dispersion was prepared by solvent evaporation method to enhance the solubility, dissolution rate and consequently, the bioavailability of Cinnarizine. These wafers were evaluated for various parameters like thickness uniformity, weight uniformity, folding endurance, swelling index, percentage moisture absorption, content uniformity, ex vivo permeation studies etc. The cumulative percentage amount of drug diffused was higher for fast releasing wafer made of 3% HPMC. The release kinetics data indicates that the release of drug from fast releasing wafer F4 follows first order release kinetics and model fits to Higuchi which is indicative of the diffusion mechanism of drug release. The mechanism of drug release was found to be non-Fickian. From all of these findings it was concluded that HPMC K4M is the best fast releasing wafer forming polymer.Keywords: Cinnarizine, Fast releasing wafers, Solid dispersion, HPMC, PVA.

COMPARATIVE EVALUATION OF SELECTED POLYMERS AND PLASTICIZER ON TRANSDERMAL DRUG DELIVERY SYSTEM

Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order.

DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE BUCCAL PATCH OF TIMOLOL MALEATE

The oral transmucosal Timolol maleate delivery bypasses liver and avoids presystemic elimination in the gastro intestinal tract andliver which enhance the bioavailability as well decreases the adverse effect. Objective: The present investigation highlights the formulation andevaluation of mucoadhesive buccal patch of Timolol maleate because Timolol maleate has biphasic solubility hence relatively permeated throughbuccal mucosa, which is well supplied with both vascular and lymphatic drainage. Material and Method: The mucoadhesive buccal patches ofTimolol maleate were prepared by solvent casting technique using polymers like Hydroxypropylmethyl cellulose-15cps and Polyvinylpyrrolidone. The formulated films were evaluated for their physiochemical parameters like surface pH, percentage moisture absorption, swellingpercentage, thickness, folding endurance and drug content. In vitro permeation and in vitro release studies were performed with pH 6.8 phosphatebuffer solution. Result and Discussion: The patches exhibited controlled release for more than 12 h. The in vitro release data were fit to differentequations and kinetic models to explain release profiles. The kinetic models used were zero order, first order higuchi’s and peppa’s. The bestmucoadhesive performance and matrix controlled release was exhibited by the formulation CK2 (3 % HPMC and 1 % PVP). Conclusion: Goodresults were obtained both in physico chemical characteristics and in vitro studies in formulation CK2. Hence the formulations of Timololmaleate bioadhesive buccal patch is a promising one as the controlled drug delivery with improved bioavailability.

Rizatriptan Transdermal Patches for the Treatment of Migraine

Transdermal patches deliver the drug through the skin in a controlled and predetermined manner in order to increase the therapeutic efficacy of drug. Rizatriptan a 2nd generation triptan that has a favorable tolerability profile and patients have reported greater satisfaction. The aim of the present work was to formulate and evaluate transdermal patches of Rizatriptan. For the current study, the transdermal patch containing drug with different ratios of polymeric combinations and varying plasticizer concentration were prepared. The patch was fabricated by solvent casting method. The casting solvents and plasticizers used were ethanol and propylene glycol respectively. The polymers used were HPMC, PVP and EC. The fabricated patches were evaluated for its physicochemical study. From the studies it concluded that F5 (EC and HPMC of 1:4 ratio and plasticizer 2 ml) whose thickness 0.124 mm, weight variation 110 mg, folding endurance 328 times, percentage moisture absorption of 5%, tensile strength of 0.78 kg/cm2, drug content of 90.42 % and in vitro drug release of 96.3 % may be selected as the optimized formulation. The released kinetics of the optimized formulation follows first order. It can be concluded that it is possible to fabricate a transdermal delivery of Rizatriptan for treatment migraine where the patient acceptance and tolerability profile is high.

Design and evaluation of guargum - based timolol maleate ocular insert For the treatment of glaucoma

Purpose: To prepare ocular inserts of timolol maleate using guar gum as a polymer for treatment of glaucoma. Methods: Timolol maleate ocular inserts were prepared by solvent casting method using guar gum in different proportions (0.25% w/v, 0.50% w/v , 75 % w/v and 1.0% w/v). The prepared formulations were evaluated for thickness, weight variation, percentage drug content, surface pH, folding endurance, percentage moisture absorption and loss, percentage swelling, mechanical strength and in vitro transcorneal permeation. In-vitro transcorneal permeation study was performed on goat cornea using modified Franz diffusion cell. Results: The inserts were found to be of uniform thickness (ranging from 41.12±0.04µm to 79.90±0.03µm) and weight (0.84±0.07 mg to 2.11±0.09 mg). The % drug content in the inserts was found to be varied between 98.69±0.58to 96.37±0.58. The cumulative % drug releases from the formulation ranged from 50.22±1.41 to 97.72±0.67over a period of 24 h. In-vitro transcorneal study revealed that an increase in concentration of polymer slows down the release of timolol maleate from the formulation. Conclusion: Ocular inserts using guar gum as a polymer were successfully prepared and can be effectively used for sustain ocular delivery over a period of 24 h.

DESIGN AND EVALUATION OF CONTROLLED-RELEASE OCULAR INSERTS OF BRIMONIDINE-TARTRATE AND TIMOLOL MALEATE

<p><strong>Objective: </strong>The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.<strong></strong></p><p><strong>Methods: </strong>Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and <em>in vitro </em>release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.<strong></strong></p><p><strong>Results: </strong>It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. <strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, <em>in vitro</em> drug release and stability.</p>

Evaluation of Porridge Made from Composite Flour of Orange-Fleshed Sweet Potato and Enset (Bulla) Flours

Bulla is the water insoluble starchy product which is separated from Kocho during the decortications process of Enset. However, this extract lacks pro-vitamin A. This study enriched the Bulla with Orange-fleshed Sweet Potato (OFSP) a plant with high levels of β-carotene that can be useful for combating vitamin A deficiency. The porridge was made of composite flours of bulla blended with 30, 35, 40 and 45% OFSP flours were investigated for proximate composition, β-carotene, functional property and sensory acceptability of products using standard methods. The data were analyzed using SAS 1.9 Software. The composite flours percentage moisture, crude (fiber, protein, fat), ash, carbohydrate, gross energy, β-carotene, pH, bulk density and water absorption capacity were found to be in the range of 29.54 to 40.25, (1.66 to 2.05, 2.11 to 2.55, 0.55 to 0.71), 1.76 to 2.11, 53.86 to 63.31, 227.49 to 268.11 Kcal/100 g, 386.68 to 558.05 μg/100 g, 4.46 to 5.71, 0.58 to 0.80 and 1.70 to 4.87 ml/g, respectively. While, the composite flours porridge percentage moisture, crude fiber, ash, crude protein, crude fat, carbohydrate, gross energy, β-carotene, pH and viscosity content found to be in the range from 43.42 to 58.03, 1.32 to 1.79, 2.39 to 2.78, 2.01 to 2.31, 0.71 to 0.82, 35.21 to 48.63, 155 to 211.11 Kcal/100 g, 201.46 to 301.50 μg/100 g, 5.71 to 5.82 and 515 to 728 cps, respectively. The porridge OB4PM2 (45% OFSP and 55% Bulla) was most preferred due to its color, odor, flavor and overall acceptability with panelist scored value of 4.28, 4.33, 4.39 and 4.45, respectively. Moreover, OB4PM2 porridge was found to be good source of ash, energy and β-carotene content.

Degradation Behaviour of Polyester/Nano-Locust Bean Pods Ash (LBPA) composite

An assessment of the degradation characteristics of LBPA reinforced polyester composite after soil burial was investigated. Nano-LBPA was prepared using a Sol - gel technique. The composite were subjected to soil burial test; the role of this test was to study the degradability, effect of microorganism present in the soil and moisture absorption on the mechanical properties of the composites. Impact, tensile, hardness and flexural properties of the composites were determined before and after soil burial tests for 30, 60 and 90days. Water absorption of the composite was studied for 24hours and their weight loss evaluated. The percentage drop in impact, tensile, flexural and hardness values after 90days exposure were approximately 42%, 34%, 65% and 23% respectively. Tensile modulus decreased approximately up to 57% and flexural modulus decreased approximately up to 41% after 90days. It was generally observed that the weight loss and percentage moisture absorption increases with increase filler loading.

The Development, Evaluation and In Vitro Release Study of the Terbinafine Transdermal Patch

Transdermal drug delivery is an alternative route for systemic drug delivery, which minimizes the absorption and increase the bioavailability. Orally Terbinafine undergoes extensive metabolism and frequent high doses are required to maintain the therapeutic level as a result, dose development toxic effect. The purpose of this research work was to formulation and evaluation of transdermal drug delivery system of Terbinafine using various polymers such as HPMC E25, Eudragit-RS100 and PVP K25 with different proportions by solvent evaporation technique. The Fourier transform infrared study revealed no physical or chemical interactions between Terbinafine and excipients. The prepared formulations were evaluated for different physicochemical characteristics such as thickness, folding endurance, drug content, percentage moisture absorption, and percentage moisture loss. The diffusion studies were performed by using modified Franz diffusion cells. The result of dissolution studies shows that formulation, SA12 showed maximum release of 92.56% in 06 h, whereas SA22 showed minimum release of 45.89% in 06 h. Based on the drug release and physicochemical values obtained the formulation SA 12 is considered as an optimized formulation, which shows higher percentage of drug release.

Development and Optimization of Controlled Release Bioerodable Anti Infective Ophthalmic Insert

The present investigation was carried out to formulate and optimize the bioerodable insert of Azithromycin in order to prolong the release time and improve the ocular availability in ophthalmic infections. A modified solvent casting method was used for the preparation of azithromycin insert in which hydroxyl propyl methyl cellulose (HPMC) and Eudragit RL100 were used as drug reservoir and rate controlling membrane respectively. Thereafter the, formulations were evaluated for the uniformity of thickness and weight, surface pH, folding endurance, percentage moisture loss, percentage moisture absorption, drug content, in-vitro release, kinetics studies (zero order, first order, Higuchi and Korsmeyer - Peppas model) and stability studies. The Formulation H8 (amongst the range of H1-H10), comprising of 1.5% HPMC and 3% Eudragit RL100, was found to be optimized formulation on the basis of uniformity of thickness (0.26±0.004 mm) and weight (24.9±0.27 mg), surface pH (7.1±0.063), folding endurance (18.3±0.81), percentage moisture loss (7.49±0.30%), percentage moisture absorption (5.7%), drug content (1.98 mg), in-vitro release (99%), AUC for in vitro and in vivo release is 38828.33 and 39783.33 g min/ml respectively and higher than pure drug (1190 g min/ml), (Shelf life- 622 days) and further better occular tolerablity found. The formulation H8 showed a steady and controlled release of the drug over a 12 hour period with non-Fickian diffusion release mechanism, compared to a normal release period of 2-3 hours. The optimized insert showed promising results and can be used to treat a wide range of ocular infections.

Design, formulation, and evaluation of novel sustain release bioadhesive in-situ gelling ocular inserts of ketorolac tromethamine.

Introduction:The eye is an interesting organ. The tear flow and blinking reflex maintains a good environment and removes foreign material from the eye. Several polymeric systems have been used to fabricate ocular inserts for better ocular bioavailability and retention to drug of which gelling systems have shown advantages of convenient administration and increased contact time.Aim:The purpose of the present study was to develop a bioadhesive in-situ gelling ocular insert of Ketorolac tromethamine using polymeric system of sodium alginate as gelling and chitosan as bioadhesive agent.Methods:Various batches of ketorolac tromethamine bioadhesive in-situ gelling ocular inserts were prepared using sodium alginate and chitosan with glycerin as a plasticizer by solvent casting method. The formulated bioadhesive in-situ gelling ocular insert were then evaluated for physical appearance, thickness, weight variation, folding endurance, percentage moisture loss, percentage moisture absorption, tensile strength, percentage flatness, bioadhesive strength, force of adhesive, drug content, in vitro drug release, sterility test, in vitro antimicrobial efficacy, and stability study.Results:The formulation F4 was shown 98.62 % drug release at the end of 12 h. Hence that F4 formulation was maximum sustain drug release than other formulation and also optimum and better result of physicochemical properties than other formulation. This optimized formulation was subjected to sterility and stability test. There was no evidence of microbial growth and hence the ocular insert passed the sterility test and there was no significant change in the physicochemical properties from 0th to 30th day. Hence, the formulation was found to be stable.Conclusion:The said promising formulation (F4) would be able to offer benefits such as increase residence time, prolonged drug release, reduction in frequency of administration and thereby definitely prove to improve the patient compliance.

Transdermal Delivery of Verapamil HCl: Effect of Penetration Agent on In Vitro Penetration through Rat Skin

Verapamil Hydrochloride is a calcium channel blocking anti-anginal agent. Extensive first pass metabolism, low bioavailability (~20%) and short biological half life (4.8 hrs) altogether makes it an ideal candidate for transdermal drug delivery. The objectives of this study were to develop matrix-type transdermal patches of verapamil hydrochloride (VPL) with combinations of hydroxypropyl methyl cellulose (HPMC) and hydroxy propyl cellulose (HPC) as matrix polymers and to investigate the influence of oleic acid (OA) on in vitro permeation of VPL through rat skin. The permeation studies were performed using Franz-type diffusion cells and full-thickness excised abdominal rat skin. The effect of the polymers on the drug release, percentage moisture loss, percentage moisture absorption, folding endurance, and thickness, were investigated.. In vitro release studies showed zero-order release of the drug from all the patches, and the mechanism of release was diffusion mediated. Data was analysed using different release kinetic models. In vitro release profiles showed that from optimized combination the release of the drug was sustained and it extended over a period of 24 hr VPM 006 emerged as the most satisfactory formulation as far as its technological properties were concerned.