Oral drug delivery remains the preferred route for administration of various drugs. Recent developments in the technology have prompted scientists to develop orally disintegrating tablets (ODTs) with improved patient compliance and convenience. ODTs are solid unit dosage forms, which disintegrate or dissolve rapidly in the mouth without chewing and water. Orally disintegrating tablets provide an advantage particularly for pediatric and geriatric populations who have difficulty in swallowing conventional tablets and capsules. This review describes the various formulation aspects, disintegrants employed and technologies developed for ODTs, along with various excipients, evaluation tests, marketed formulations, and drugs explored in this field.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Topical application of drugs to the eye is most popular and well-accepted route of administration for the treatment of various eye disorders. A variety of ocular dosage form and drug delivery systems, including a controlled release of the drug, drug targeting, and penetration enhancement of the drug, have been investigated. Polymers have been widely used as the drug carrier for controlled-release systems. Polymers release the drug as they themselves degrade and are sometimes finally absorbed within the body. In this article, several ocular drug delivery systems have discussed using different kinds of polymers and their acceptance over conventional.

[ABSTRACT]  [FULL TEXT]  [PDF]

Cosmetics have become part of our routine. Their use has increased significantly in recent years however the continuous use of cosmetics over prolonged time may result into various undesirable effects, which may be serious at times. This review is an attempt to trace out the history of cosmetics used by different civilizations over centuries

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Fast-dissolving tablets (FDT) of promethazine theoclate were prepared by direct-compression method after incorporating superdisintegrants Ac-Di-Sol, Sodium Starch Glycolate (SSG), and Crospovidone in different concentrations. Nine formulations having superdisintegrants at different concentration levels were prepared to assess their efficiency and critical concentration level. Different types of evaluation parameters for tablets were used. Tablets containing Ac- Di- Sol showed superior organoleptic properties, along with excellent in vitro and in vivo dispersion time and drug release, as compared to other formulations.

[ABSTRACT]  [FULL TEXT]  [PDF]

The objective of the present study was to microencapsulate the anti-inflammatory drug (aceclofenac) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track. The drug was targeted to the colon and their aligned area for their local effect. Aceclofenac was microencapsulated with Eudragit (S 100, RL 100, and RS 100), using an O/W emulsion-solvent evaporation technique. Aceclofenac microspheres were subjected to micromeritic properties including angle of repose, bulk density, tapped density, Carr's index, Hausner's ratio, and particle size determination. Microspheres were subjected to drug loading, in vitro drug release as well as for scanning electron microscopy. The prepared microspheres were white, free-flowing, and almost spherical in shape. The drug-loaded microspheres show 60-82% drug entrapment, angle of repose was in the range of 16.13 ± 0.621-24 ± 0.590, bulk and tapped densities respectively were in the range of 0.311 ± 0.006-0.562 ± 0.012 and 0.373 ± 0.01-0.735 ± 0.02, Carr's index ranges from 14.04 ± 0.026 to 27.25 ± 1.405, Hausner's ratio was 1.14 ± 0.026-1.37 ± 0.03, and particle size was in the range of 79.7016-144.840 µm. In vitro drug release studies were carried out up to 24 h in three different pH media, i.e., 0.1 N HCl (pH 1.2), phosphate buffer (pH 6.8), and phosphate buffer (pH 7.4). The drug-polymer concentration of dispersed phase influences the particle size and drug release properties. All the formulations at higher pH were followed by the Matrix-Higuchi model.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

The biopharmaceutical classification system (BCS) is a new concept in the field of pharmaceutical science and technology. This is a valuable tool for the formulation scientists, for the selection and design of the formulation of any drug substance. The recent developments have also enabled us to predict the solubility and permeability characteristics of the drug molecule in the early development stages so that the necessary structural changes can be made to the molecule in order to optimize the pharmacokinetic parameters. The BCS has also got a place in various guidance documents of regulatory importance. This article reviews the criteria for classifying drugs according to the BCS and discusses further potential applications of the BCS, including the developments of new drugs and controlled release products.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]

Glass transition temperature (Tg) is an important tool used to modify physical properties of drug and polymer molecules. Tg is shown by certain crystalline as well as amorphous solids. During the process of heating, some solid gets melted and if quench cooled, instead of crystallizing, gets converted to amorphous solid form appearing as that of glass. This glass formation is seen because of the dynamic arrest of molecules forming a disordered state at Tg. The molecules/atoms in glassy state are subject to only vibration and not translational and rotational motion. Mainly, at Tg, conversion of glassy (vitrified, amorphous) solid to rubbery (viscous liquid) takes place. Numerous factors like structural change in molecules, cooling rate and incorporation of additives alter the Tg. Techniques like differential scanning calorimetry, elastic modulus, broad-line NMR are used to measure the Tg of substances. The change in Tg has been carried out to improve dissolution and bioavailability, processing and handling qualities of the material.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]

Cosmetics are incredible in demand since historical time till day. Lipstick formulations are most widely used to enhance the beauty of lips and to add glamor's touch to the makeup. It is difficult to apply lipsticks to the dried, chafed, chapped, cracked lips with sores and lesions. In such cases, one can use medicated lipsticks for the purpose of curing topical infections and beautification of lips. With this aim and objectives, an attempt was made to formulate medicated lipstick by using cow ghee and honey as natural excipients that substituted synthetic ingredients like isopropyl myristate, lanolin, cetyl alcohol, and castor oil. Allantoin was selected a model drug for the local action on lips. In vitro evaluation was done on bovine lip membrane, and the data suggested that the drug remained on the membrane only and did not diffuse through the membrane in diffusion studies for 8 h. After 8 h, 0.16% drug release was observed till 12 h. Thus, allantoin can remain topically on lips for 8 h without showing any systemic effects. The lipsticks were evaluated for their organoleptic properties such as spreading, covering property, hardness, shine, and gloss and found to be satisfactory product to give attractive beauty with therapeutic effect on the diseased lips. Thus, the medicated lipsticks with the natural ingredients like cow ghee and honey can serve as economical and effective cosmoseutical product.

[ABSTRACT]  [FULL TEXT]  [PDF]

The present research work investigates enhancement of dissolution profile of meloxicam using solid dispersion (SD) with various polymers. The work also describes the formulation of dispersible tablet (DT) and effervescent tablet of meloxicam. PEG 6000, PEG 8000, PEG 20000, Lutrol F-127, and β -cyclodextrin were selected for the preparation of SD. The SDs were prepared by melting and solvent evaporation methods. Dissolution studies were performed for plain meloxicam, SDs, and tablet formulations. Infrared spectroscopy and differential scanning calorimetry were performed to identify the physicochemical interaction between drug and carriers. Dispersible tablets and effervescent tablets were compared with tablet containing plane drug for dissolution profile. Dissolution of DT improved significantly in SD product (<95% in 1 min).

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Solubility is an essential factor for drug effectiveness, independent of the route of administration. Poorly soluble drugs are often a challenging task for formulators in the industry. Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non-aqueous media. Nanosuspension technology can be used to improve the stability as well as the bioavailability of poorly soluble drugs. Nanosuspensions are biphasic systems consisting of pure drug particles dispersed in an aqueous vehicle, stabilized by surfactants. These are simple to prepare and are more advantageous than other approaches. Techniques such as wet milling, high-pressure homogenization, emulsification-solvent evaporation and super critical fluid have been used in the preparation of nanosuspensions. It has the advantage of delivery by various routes, including oral, parenteral, pulmonary and ocular routes. The present article reviews the current methods used to prepare nanosuspensions and their application in drug delivery.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Ocular diseases require localized administration of drugs to the tissues around the ocular cavity. The existing ocular drug delivery systems are fairly primitive and inefficient. However, the design of ocular system is undergoing gradual transition from an empirical to rational basis. In the recent years, there has been explosion of interest in the polymer based delivery devices. Utilization of the principles of controlled release as embodied by ocular inserts offers an attractive approach to the problem of prolonging pre-corneal drug residence times. In the present update, the authors discuss the basic concept of ocular inserts as drug delivery system and examine the few inserts, which are available in the market or are being developed by pharmaceutical companies for drug delivery. The article discusses soluble ocular drug insert (SODI), Ocusert, Collagen Shields, Ocufit, Minidisc and new ophthalmic delivery system (NODS) with special attention to biological/clinical performances, and potential for future applications and developments.

[ABSTRACT]  [FULL TEXT]  [PDF]

Pulsatile drug delivery system is the most interesting time- and site-specific system. This system is designed for chronopharmacotherapy which is based on circadian rhythm. The principle rationale for the use of pulsatile release is for the drugs where a constant drug release, i.e., a zero-order release is not desired. Pulsatile drug delivery system is defined as the rapid and transient release of certain amount of molecules within a short time period immediately after a predetermined off-release period, i.e., lag time. Various systems like capsular systems, osmotic systems, pulsatile system based on the use of soluble or erodible polymer coating, use of rupturable membranes and pulsatile system based on membrane permeability are summarized in this article. These systems are beneficial for the drugs having chronopharmacological behavior where night time dosing is required and for the drugs having high first-pass effect and having specific site of absorption in gastrointestinal tract.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

With the discovery of insulin in 1922, identification and commercialization of potential protein and peptide drugs have been increased. Since then, research and development to improve the means of delivering protein therapeutics to patients has begun. The research efforts have followed two basic pathways: One path focused on noninvasive means of delivering proteins to the body and the second path has been primarily aimed at increasing the biological half-life of the therapeutic molecules. The search for approaches that provide formulations that are stable, bioavailable, readily manufacturable, and acceptable to the patient, has led to major advances in the development of nasal and controlled release technology, applicable to every protein or peptide. In several limited cases, sustained delivery of peptides and proteins has employed the use of polymeric carriers. More successes have been achieved by chemical modification using amino acid substitutions, protein pegylation or glycosylation to improve the pharmacodynamic properties of certain macromolecules and various delivery systems have been developed like the prolease technology, nano-particulate and microparticulate delivery systems, and the mucoadhesive delivery of peptides. The needle and syringe remain the primary means of protein delivery. Major hurdles remain in order to overcome the combined natural barriers of drug permeability, drug stability, pharmacokinetics, and pharmacodynamics of protein therapeutics. In our present review we have tried to compile some recent advances in protein and peptide drug delivery systems.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]

There is considerable interest in the skin as a site of drug application for both local and systemic effect. However, the skin, in particular the stratum corneum, possesses a formidable barrier to drug penetration thereby limiting topical and transdermal bioavailability. Skin penetration enhancement techniques have been developed to improve bioavailability and to increase the range of drugs for which topical and transdermal delivery is a viable option. The permeation of drug through skin can be enhanced by both chemical penetration enhancement and physical methods. In this review, we have discussed the physical and chemical penetration enhancement technology for transdermal drug delivery as well as the probable mechanisms of action.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]

Matrix-type transdermal drug delivery systems of haloperidol lactate were prepared using different ratios of ethyl cellulose (EC):polyvinyl pyrrolidone (PVP) (3:2, 2:3, 4:1, 1:2, 2:1, and 1:4) by solvent-evaporation technique. Physicochemical parameters were characterized, and dissolution studies of the formulated films were performed. In addition, solubility studies at various values of pH were carried out, and partition coefficient in octanol/water system, flux, and enhancement ratio were also evaluated. In vitro permeation studies were done using modified Franz diffusion cells through human cadaver skin utilizing 20% PEG 400 in normal saline. Permeation studies illustrated that 4% hyaluronidase enzyme was a good enhancer. The prepared films were subjected to scanning electron microscopy (SEM) and fourier transform infrared spectroscopy (FT-IR) spectral analysis. Higuchi and Peppas models were used for optimizing the formulation.

[ABSTRACT]  [FULL TEXT]  [PDF]

The purpose of this research was to formulate and optimize an effervescent floating tablet formulation of salbutamol sulfate using full factorial design. Salbutamol sulfate has an absorption window in the stomach and in the upper part of the small intestine. A 3 ² full factorial design (eight runs) was utilized to optimize the formulation wherein the content of hydroxylpropyl methyl cellulose (HPMC) (X ₁ ) and sodium bicarbonate (X ₂ ) were taken as independent variables and % drug release after 6 h (Y ₁ ), t _50% (Y ₂ ), and buoyancy lag time (BLT) (Y ₃ ) were taken as the dependent variables. Salbutamol sufate, HPMC K4M and HPMC K100M CR, stearic acid, talc, dicalcium phosphate, polyvinyl pyrrolidone, and magnesium stearate were used for the current research work. Two viscosity grades of HPMC as matrix materials were used for formulating the tablets, which were prepared by wet granulation. The release data were evaluated by the model-dependent (curve fitting) method using the PCP Disso v2.08 software. Optimization studies were carried out using the Design Expert Software (Version 7.0.3). The in vitro drug release mechanism showed anomalous transport. An increase in the concentration and viscosity grade of the polymer resulted in a decrease in the release rate, but it was found that at a higher concentration of HPMC, the viscosity grade did not significantly affect the drug release. Concentration of both HPMC and sodium bicarbonate had a significant effect on the BLT. Optimized effervescent floating tablets of salbutamol sulfate were successfully prepared and a good correlation was observed between predicted and actual values of the dependent variables chosen for the study. Viscosity grade of HPMC did not significantly impact the floatability of the dosage form. Thus, we can conclude that a combination of HPMC, stearic acid, and sodium bicarbonate can be used to increase the gastric residence time of the dosage form up to 12 h.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]

Poly (D, L-lactide-co-glycolide) (PLGA) is approved by the Food and Drug Administration for drug delivery use. The polymeric nanoparticles based on PLGA and its co-polymer are designed for controlled and targeted drug delivery. Also, PLGA and its co-polymer are important in designing nanoparticles with desired characteristics such as biocompatibility, biodegradation, particle size, surface properties, drug release and targetability. This review focuses on the polymer literature, methods for preparation of nanoparticles and recent studies on the nanoparticles based on PLGA and its co-polymer for the conventional and targeted delivery of drugs by various routes.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Itraconazole is practically insoluble in water; large interindividual and intraindividual variations of its oral bioavailability are reported. A mucoadhesive drug delivery system is useful to prolong the retention time of a dosage form in the stomach, thereby improving the oral bioavailability of the drug. Solid dispersion of itraconazole with Eudragit E100 was prepared by spray-drying method to improve dissolution. Trilayered mucoadhesive tablet was prepared, with inner core containing solid dispersion of the drug and with carbopol and HPMC sandwiched between two layers of hydrophilic mucoadhesive polymer mixture of carbopol and Hydroxypropyl methyl cellulose (HPMC). Amounts of Carbopol 934P (CP) and Methocel K4M (HPMC) were varied in the outer coat around the solid dispersion. The drug-release pattern for all the formulation combinations was found to be nonfickian, approaching zero-order kinetics. Suitable combination of two polymers provided adequate bioadhesive strength and sustained-release profile with zero-order kinetics.

[ABSTRACT]  [FULL TEXT]  [PDF]

The purpose of the study was to prolong the gastric residence time of atenolol by designing its floating tablets and to study the influence of different polymers on its release rate. Nine formulations of atenolol containing varying concentrations of polymers were designed by optimization. The floating matrix tablets of atenolol were prepared by direct compression method. The prepared tablets were evaluated for physicochemical parameters such as hardness, floating properties (floating lag time, floating time and matrix integrity), swelling studies and drug content. The physicochemical parameters of formulated tablets were found to be within normal range. A significant difference in drug release (P < 0.0001) and floating lag time ( P < 0.005) at 0.5, one, four and eight hours were observed. The floating lag time of all the formulations was within the prescribed limit (<10 minutes). All the formulations showed good matrix integrity and retarded the release of drug for eight hours. The release pattern of atenolol was fitted to different models based on coefficient of correlation (r). All the formulations, except F2, F3 and F6 showed Korsemeyer-Peppas model as the best fit model. Formulation F2 and F3 showed first order model while F6 showed zero order model. Diffusion exponent (n) value was found in the range of 0.52-0.99 indicating diffusion as a release mechanism. The swelling studies of all the formulations showed that formulations containing Xanthan gum has higher swelling indices than HPMC K100M and HPMC K4M. It can be concluded that formulations with higher swelling indices retarded the release of drugs more than those with lower swelling indices.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Terbinafine HCl (Poorly water soluble drug), when prepared as solid dispersion showed improved solubility and dissolution. So the main purpose of this investigation was to increase the solubility and dissolution rate of Terbinafine HCl by the preparation of its solid dispersion with polyvinyl pyrrolidone K30 using solvent evaporation methods. FT- IR spectra revealed no chemical incompatibility between drug and polyvinyl pyrrolidone K30. Drug-polymer interactions were investigated using differential scanning calorimetry (DSC), Powder X-Ray Diffraction (PXRD).

[ABSTRACT]  [FULL TEXT]  [PDF]

The present work is to formulate effective hand rub disinfectant by selecting broad-spectrum antimicrobial and antifungal agents. Increased need of easy-to-use hand rub disinfectant in pharmaceutical, food processing industry, hospitals, and in clinical labs necessitated development of the best possible product. Formulations were prepared using Benzalkonium chloride, chlorhexidine gluconate as potent disinfectants along with alcohol 70%. In low concentration they were highly effective without leaving any toxic effect on the user's skin. A synergistic effect was observed when ethyl alcohol 70% was used in combination. Suitable emollient and skin conditioning agents were used to avoid possible dehydrating effect on the user's skin. Excellent volatility of the preparation was observed after use, leaving a thin antimicrobial film on the user's hand. The use of suitable excipient brought effective removal of after the use leaving a soothening effect on the skin. The aim of present work is to develop hand rub formulation which evaporates quickly after applications leaving no trace on hands as in case of hand rub gels. The present formulation was found to be effective when compared with marketed liquid hand rub.

[ABSTRACT]  [FULL TEXT]  [PDF]

Size reduction is a process of reducing large solid unit masses into small unit masses, coarse particles or fine particles. Size reduction process is also termed as comminution or diminution or pulverizations . In addition to the standard adjustments of the milling process (i.e., speed, screen size, design of rotor, load), special techniques of milling may be useful including special atmosphere, temperature control, sonocrystallization, supercritical fluid process. etc. Moreover, some advance technologies of size reduction including Micron Technologies, Gran-U-Lizer™ Technology, Jet-O-Mizer™ and Microfluidics® have been popular. Various application of size reduction concept covers oral delivery of poorly soluble drugs, micronization, nanotechnology (micro- and nano suspensions), etc. This systemic review highlights advantages and disadvantages, mechanisms, theories, techniques, advances, and pharmaceutical applications of size reduction technology.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Transdermal systems are ideally suited for diseases that demand chronic treatment. Hence, an anti-diabetic agent of both therapeutic and prophylactic usage has been subjected to transdermal investigation. Gliclazide, a second-generation hypoglycemic agent, faces problems like its poor solubility, poor oral bioavailability with large individual variation and extensive metabolism. In the present work, transdermal matrix-type patches were prepared by film casting techniques on mercury using polymers like HPMC, Eudragit RL-100, and chitosan. Also an attempt was made to increase the permeation rate of drug by preparing an inclusion complex with hydroxypropyl β-cyclodextrin (HP β-CD). The possibility of a synergistic effect of chemical penetration enhancers (CPE) (propylene glycol and oleic acid) on the transdermal transport of the drug was also studied. Folding endurance was found to be high in patches containing higher amount of the Eudragit. There was increase in tensile strength with an increase in Eudragit in the polymer blend. In vitro drug release profile indicates that the drug release is sustained with increasing the amount of Eudragit in patches. The patches containing inclusion complex of drug showed higher permeation flux compared with patches containing plain drug. The result of the synergistic effect indicates that the HP β- CD in conjunction with other CPE showed a higher permeation flux.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub]

Roxithromycin is a broad spectrum, semisynthetic macrolide antibiotic, having bitter taste. In the present study, an attempt has been made to mask the bitter taste of roxithromycin by complexation technique. Weak cation exchange resins Indion 214 and Amberlite IRP64, polymer carbopol 934P were used in formulation of complexes with the drug. The loading process was optimized for the pH of loading solution and resin or polymer:drug ratio. The complexes were evaluated for bulk density, angle of repose, taste masking, and in vitro drug release. In vitro drug release studies showed more than 80% drug release from the optimized formulation within 30 min. Amberlite IRP64 was found to be better complexing agent for masking the bitter taste of roxithromycin.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

The effect of HPMC on solubility and dissolution of carbamazepine form III (CBZ) was investigated in 50% w/w of CBZ form III in HPMC solid dispersion and physical mixture. Powdered samples of CBZ form III, physical mixture, and solid dispersion were characterized for thermal behavior (DSC), crystallinity (PXRD), and compatibility (FT-IR). Solubility and dissolution studies were carried out in different simulated gastrointestinal fluids and de-ionized water. Solubility studies in simulated gastric fluid (SGF) revealed that acidic pH favors formation of CBZ dihydrate. Triton X 100 in blank fast-state simulated gastric fluid (FaSSGF) prevents the formation of CBZ dihydrate in acidic pH. A maximum solubility of 268.77 µg/mL was achieved with fed-state simulated intestinal fluid (FeSSIF). Correlation between solubility and pH could not be established. Both solubility and dissolution studies revealed that HPMC had a profound effect of enhancement of solubility and dissolution of CBZ form III in both physical mixtures and solid dispersions. HPMC prevents the formation of CBZ dihydrate and thereby improves the solubility and dissolution. This was further correlated with results obtained from DSC and XRD. There was no drastic difference in solubility and dissolution of CBZ form III with different media. It was observed that there was no existing relationship between solubility and dissolution of CBZ form III in different media.

[ABSTRACT]  [FULL TEXT]  [PDF]